Avapritinib – Uses, Dosage, Side Effects, Interactions

Mechanism of Action
Indications
Contraindications
Dosage
Side Effects
Drug Interactions
Pregnanct and Lactations
How should this medicine be used?
What special precautions should I follow?

Avapritinib is an orally bioavailable inhibitor of specific mutated forms of platelet-derived growth factor receptor alpha (PDGFR alpha; PDGFRa) and mast/stem cell factor receptor c-Kit (SCFR), with potential antineoplastic activity. Upon oral administration, avapritinib specifically binds to and inhibits specific mutant forms of PDGFRa and c-Kit, including the PDGFRa D842V mutant and various KIT exon 17 mutants. This results in the inhibition of PDGFRa- and c-Kit-mediated signal transduction pathways and the inhibition of proliferation in tumor cells that express these PDGFRa and c-Kit mutants. PDGFRa and c-Kit, protein tyrosine kinases and tumor-associated antigens (TAAs), are mutated in various tumor cell types; they play key roles in the regulation of cellular proliferation.

Avapritinib, or BLU-285, is a selective tyrosine kinase inhibitor of KIT and platelet-derived growth factor receptor alpha indicated for the treatment of unresectable, metastatic gastrointestinal stromal tumors. It is one of the first medications available for the treatment of multidrug-resistant cancers. Avapritinib shares a similar mechanism with [ripretinib]. Avapritinib was granted FDA approval on 9 January 2020.

Avapritinib is a Kinase Inhibitor. The mechanism of action of avapritinib is as a Tyrosine Kinase Inhibitor, Cytochrome P450 2C9 Inhibitor, and P-Glycoprotein Inhibitor, Breast Cancer Resistance Protein Inhibitor, Multidrug and Toxin Extrusion Transporter 1 Inhibitor, and Multidrug and Toxin Extrusion Transporter 2 K Inhibitor, and Bile Salt Export Pump Inhibitor.

Mechanism of Action

Avapritinib has a negative modulating effect on the transporters ABCB1 and ABCG2, which mediate the multidrug resistance phenotype of some cancers. This modulation may be due to interactions of avapritinib with the drug-binding pocket of these transporters. Negative modulation of these transporters resensitizes cancerous cells to treatment with chemotherapeutic agents like [paclitaxel].

Avapritinib is a selective kinase inhibitor that negatively modulates the action of cell transporters to resensitize them to other chemotherapies. It has a long duration of action as it is given once daily. Patients should be counseled regarding the risk of intracranial hemorrhage, CNS effects, and embryo-fetal toxicity.

Indications

Avapritinib is indicated for the treatment of unresectable, metastatic gastrointestinal stromal tumors with platelet-derived growth factor receptor alpha exon 18 mutations.
Treatment of mastocytosis
Treatment of all conditions included in the category of malignant neoplasms (except hematopoietic and lymphoid tissue neoplasms)
Ayvakyt is indicated as monotherapy for the treatment of adult patients with unresectable or metastatic gastrointestinal stromal tumors (GIST) harboring the platelet-derived growth factor receptor alpha (PDGFRA) D842V mutation.
Avapritinib is indicated for the treatment of adults with unresectable or metastatic GIST harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations.^[rx]It is also used to treat adult patients with advanced systemic mastocytosis (AdvSM). AdvSM includes patients with aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematological neoplasm (SM-AHN), and mast cell leukemia. However, it is not recommended for the treatment of patients with AdvSM with platelet counts of less than 50 X 10⁹ L.^[rx]
Advanced Systemic Mastocytosis (AdvSM)
Mast Cell Leukemia (MCL)
Metastatic Gastrointestinal Stromal Tumor
Systemic Mastocytosis With an Associated Hematological Neoplasm
Unresectable Gastrointestinal stromal tumor

Use in Cancer

Avapritinib is approved to treat adults with:

A gastrointestinal stromal tumor (GIST) that cannot be removed by surgery or has metastasized (spread to other parts of the body) and has certain mutations in the PDGFRA gene.
Systemic mastocytosis that is advanced, including the following types:
- Aggressive systemic mastocytosis.
- Systemic mastocytosis with an associated hematologic neoplasm (SM-AHN).
- Mast cell leukemia. Avapritinib is not recommended for the treatment of advanced systemic mastocytosis in people with low platelet counts (less than 50 × 109/L).

Avapritinib is also being studied in the treatment of other conditions and other types of cancer.

Contraindications

The following conditions are contraindicated with this drug. Check with your physician if you have any of the following:

decreased blood platelets
bleeding within the skull
pregnancy
a patient who is producing milk and breastfeeding

Dosage

Strengths: 100 mg; 200 mg; 25 mg; 300 mg; 50 mg

Stomach Cancer

300 mg orally once a day until disease progression or unacceptable toxicity

Renal Dose Adjustments

Mild (60 to less than 90 mL/min) to moderate (30 to less than 60 mL/min) renal impairment: No adjustment recommended.
Severe (15 to less than 30 mL/min) or end-stage (less than 15 mL/min) renal impairment: Data not available

Liver Dose Adjustments

Mild (total bilirubin less than or equal to upper limit of normal [ULN] and aspartate aminotransferase [AST] greater than ULN or total bilirubin greater than 1 to 1.5 times ULN and any AST) or moderate (total bilirubin greater than 1.5 to 3 x ULN and any AST) hepatic impairment: No adjustment recommended.
Severe hepatic impairment: Data not available

Dose Adjustments

RECOMMENDED DOSE REDUCTIONS:

First dose reduction: 200 mg orally once a day
Second dose reduction: 100 mg orally once a day
Permanently discontinue therapy in patients unable to tolerate 100 mg orally once a day.

RECOMMENDED DOSE REDUCTIONS FOR ADVERSE REACTIONS:
INTRACRANIAL HEMORRHAGE:
Grade 1 or 2:

First occurrence: Withhold this drug until resolution; resume at reduced dose.
Subsequent occurrence: Permanently discontinue this drug.

Grade 3 or 4:

Permanently discontinue this drug.

CENTRAL NERVOUS SYSTEM EFFECTS:

Grade 1: Continue at same dose or withhold until improvement to baseline or resolution; resume at same OR reduced dose.
Grade 2 or 3: Withhold this drug until improvement to baseline, Grade 1, or resolution; resume at same OR reduced dose.

Grade 4:

Permanently discontinue therapy.

Side Effects

The Most Common

stomach pain
vomiting
nausea
diarrhea
heartburn
headache
tiredness
difficulty falling asleep or staying asleep
hair loss
hair color changes
weight loss
teary eyes
taste changes
swelling of face, eyes, mouth, or throat
swelling of hands, ankles, or feet
vomiting blood or material that looks like coffee grounds or red or tarry black stools
severe headache, vomiting, confusion, vision problems, drowsiness, extreme tiredness, or weakness on one side of your body
forgetfulness, confusion, drowsiness, dizziness, difficulty sleeping, difficulty speaking, hallucinations, or changes in mood or behavior
rash
shortness of breath
fever or other signs of infection

More Common

a severe headache, vision problems;
unusual changes in mood or behavior;
problems with speech, thinking, or memory;
confusion, hallucinations (seeing objects or hearing things that are not real);
severe drowsiness or dizziness;
trouble sleeping; or
severe weakness on one side of your body.
nausea, vomiting, loss of appetite, stomach pain;
diarrhea, constipation;
fluid retention, swelling;
feeling dizzy, weak, or tired;
muscle weakness;
watery eyes;
rash; or
hair color changes.

Rare

Agitation
black, tarry stools
bloody stools
chest pain
chills
confusion
constipation
cough
decreased awareness or responsiveness
decreased urine output
depressed mood
difficult, burning, or painful urination
dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
dry skin and hair
dilated neck veins
fainting
feeling cold
fever
frequent urge to urinate
gaseous stomach pain
hair loss
hoarseness or husky voice

Drug Interactions

DRUG	INTERACTION
Abaloparatide	The therapeutic efficacy of Abaloparatide can be decreased when used in combination with Avapritinib.
Abametapir	The serum concentration of Avapritinib can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Avapritinib can be increased when combined with Abatacept.
Abrocitinib	The metabolism of Abrocitinib can be decreased when combined with Avapritinib.
Acenocoumarol	The metabolism of Acenocoumarol can be decreased when combined with Avapritinib.
Acetaminophen	The serum concentration of Acetaminophen can be increased when it is combined with Avapritinib.
Acetohexamide	The metabolism of Acetohexamide can be decreased when combined with Avapritinib.
Acetyl sulfisoxazole	The metabolism of Avapritinib can be decreased when combined with Acetyl sulfisoxazole.
Acetylsalicylic acid	The metabolism of Acetylsalicylic acid can be decreased when combined with Avapritinib.
Adalimumab	The metabolism of Avapritinib can be increased when combined with Adalimumab.
Agomelatine	The metabolism of Avapritinib can be decreased when combined with Agomelatine.
Alosetron	The metabolism of Alosetron can be decreased when combined with Avapritinib.
Alpelisib	The serum concentration of Avapritinib can be decreased when it is combined with Alpelisib.
Aminophenazone	The metabolism of Aminophenazone can be decreased when combined with Avapritinib.
Amiodarone	The metabolism of Avapritinib can be decreased when combined with Amiodarone.
Amitriptyline	The metabolism of Amitriptyline can be decreased when combined with Avapritinib.
Amodiaquine	The metabolism of Avapritinib can be decreased when combined with Amodiaquine.
Amprenavir	The metabolism of Avapritinib can be decreased when combined with Amprenavir.
Anakinra	The metabolism of Avapritinib can be increased when combined with Anakinra.
Antipyrine	The metabolism of Antipyrine can be decreased when combined with Avapritinib.
Apalutamide	The metabolism of Avapritinib can be increased when combined with Apalutamide.
Apixaban	The metabolism of Apixaban can be decreased when combined with Avapritinib.
Apremilast	The metabolism of Avapritinib can be increased when combined with Apremilast.
Aprepitant	The metabolism of Avapritinib can be decreased when combined with Aprepitant.
Arformoterol	The metabolism of Arformoterol can be decreased when combined with Avapritinib.
Armodafinil	The metabolism of Avapritinib can be decreased when combined with Armodafinil.
Artemether	The metabolism of Artemether can be decreased when combined with Avapritinib.
Asciminib	The metabolism of Avapritinib can be decreased when combined with Asciminib.
Asunaprevir	The metabolism of Asunaprevir can be decreased when combined with Avapritinib.
Atazanavir	The metabolism of Avapritinib can be decreased when combined with Atazanavir.
Atovaquone	The metabolism of Avapritinib can be decreased when combined with Atovaquone.
Avanafil	The serum concentration of Avanafil can be increased when it is combined with Avapritinib.
Avatrombopag	The metabolism of Avapritinib can be increased when combined with Avatrombopag.
Azelastine	The metabolism of Azelastine can be decreased when combined with Avapritinib.
Berotralstat	The metabolism of Avapritinib can be decreased when combined with Berotralstat.
Bexarotene	The metabolism of Bexarotene can be decreased when combined with Avapritinib.
Bimekizumab	The metabolism of Avapritinib can be increased when combined with Bimekizumab.
Boceprevir	The metabolism of Avapritinib can be decreased when combined with Boceprevir.
Bortezomib	The metabolism of Bortezomib can be decreased when combined with Avapritinib.
Bosentan	The metabolism of Avapritinib can be increased when combined with Bosentan.
Brivaracetam	The metabolism of Brivaracetam can be decreased when combined with Avapritinib.
Buprenorphine	The metabolism of Buprenorphine can be decreased when combined with Avapritinib.
Bupropion	The metabolism of Bupropion can be decreased when combined with Avapritinib.
Cabozantinib	The metabolism of Cabozantinib can be decreased when combined with Avapritinib.
Canakinumab	The metabolism of Avapritinib can be increased when combined with Canakinumab.
Candesartan cilexetil	The metabolism of Candesartan cilexetil can be decreased when combined with Avapritinib.
Cannabidiol	The metabolism of Cannabidiol can be decreased when combined with Avapritinib.
Capecitabine	The metabolism of Capecitabine can be decreased when combined with Avapritinib.
Carbamazepine	The metabolism of Avapritinib can be increased when combined with Carbamazepine.
Carbimazole	The therapeutic efficacy of Carbimazole can be decreased when used in combination with Avapritinib.
Carvedilol	The metabolism of Carvedilol can be decreased when combined with Avapritinib.
Celecoxib	The metabolism of Celecoxib can be decreased when combined with Avapritinib.
Cenobamate	The serum concentration of Avapritinib can be decreased when it is combined with Cenobamate.
Ceritinib	The metabolism of Avapritinib can be decreased when combined with Ceritinib.
Cerivastatin	The metabolism of Avapritinib can be decreased when combined with Cerivastatin.
Certolizumab pegol	The metabolism of Avapritinib can be increased when combined with Certolizumab pegol.
Chlorpropamide	The metabolism of Chlorpropamide can be decreased when combined with Avapritinib.
Cimetidine	The metabolism of Avapritinib can be decreased when combined with Cimetidine.
Cinnarizine	The metabolism of Cinnarizine can be decreased when combined with Avapritinib.
Ciprofloxacin	The metabolism of Avapritinib can be decreased when combined with Ciprofloxacin.
Clarithromycin	The metabolism of Avapritinib can be decreased when combined with Clarithromycin.
Clevidipine	The metabolism of Avapritinib can be decreased when combined with Clevidipine.
Clopidogrel	The metabolism of Avapritinib can be decreased when combined with Clopidogrel.
Clozapine	The metabolism of Avapritinib can be decreased when combined with Clozapine.
Cobicistat	The metabolism of Avapritinib can be decreased when combined with Cobicistat.
Conivaptan	The metabolism of Avapritinib can be decreased when combined with Conivaptan.
Crizotinib	The metabolism of Avapritinib can be decreased when combined with Crizotinib.
Curcumin	The metabolism of Avapritinib can be decreased when combined with Curcumin.
Cyclizine	The metabolism of Avapritinib can be decreased when combined with Cyclizine.
Cyclophosphamide	The metabolism of Cyclophosphamide can be decreased when combined with Avapritinib.
Cyclosporine	The metabolism of Avapritinib can be decreased when combined with Cyclosporine.
Dabrafenib	The serum concentration of Avapritinib can be decreased when it is combined with Dabrafenib.
Dacomitinib	The metabolism of Dacomitinib can be decreased when combined with Avapritinib.
Danazol	The metabolism of Avapritinib can be decreased when combined with Danazol.
Dapagliflozin	The metabolism of Dapagliflozin can be decreased when combined with Avapritinib.
Dapsone	The metabolism of Dapsone can be decreased when combined with Avapritinib.
Darunavir	The metabolism of Avapritinib can be decreased when combined with Darunavir.
Delafloxacin	The metabolism of Avapritinib can be increased when combined with Delafloxacin.
Delavirdine	The metabolism of Avapritinib can be decreased when combined with Delavirdine.
Desogestrel	The metabolism of Desogestrel can be decreased when combined with Avapritinib.
Desvenlafaxine	The metabolism of Avapritinib can be decreased when combined with Desvenlafaxine.
Dexamethasone	The metabolism of Avapritinib can be increased when combined with Dexamethasone.
Dexibuprofen	The metabolism of Dexibuprofen can be decreased when combined with Avapritinib.
Dextromethorphan	The metabolism of Dextromethorphan can be decreased when combined with Avapritinib.
Diacerein	The metabolism of Avapritinib can be decreased when combined with Diacerein.
Diazepam	The metabolism of Diazepam can be decreased when combined with Avapritinib.
Diclofenac	The metabolism of Diclofenac can be decreased when combined with Avapritinib.
Dicoumarol	The metabolism of Dicoumarol can be decreased when combined with Avapritinib.
Diethylstilbestrol	The metabolism of Avapritinib can be decreased when combined with Diethylstilbestrol.
Diltiazem	The metabolism of Avapritinib can be decreased when combined with Diltiazem.
Diosmin	The metabolism of Avapritinib can be decreased when combined with Diosmin.
Diphenhydramine	The metabolism of Diphenhydramine can be decreased when combined with Avapritinib.
Doconexent	The metabolism of Avapritinib can be decreased when combined with Doconexent.
Donepezil	The metabolism of Donepezil can be decreased when combined with Avapritinib.
Doxazosin	The metabolism of Doxazosin can be decreased when combined with Avapritinib.
Doxepin	The metabolism of Doxepin can be decreased when combined with Avapritinib.
Dronabinol	The serum concentration of Dronabinol can be increased when it is combined with Avapritinib.
Dronedarone	The metabolism of Avapritinib can be decreased when combined with Dronedarone.
Duloxetine	The metabolism of Duloxetine can be decreased when combined with Avapritinib.
Efavirenz	The metabolism of Avapritinib can be decreased when combined with Efavirenz.

Eletriptan	The metabolism of Eletriptan can be decreased when combined with Avapritinib.
Elvitegravir	The metabolism of Avapritinib can be decreased when combined with Elvitegravir.
Emapalumab	The metabolism of Avapritinib can be increased when combined with Emapalumab.
Enasidenib	The metabolism of Enasidenib can be decreased when combined with Avapritinib.
Enzalutamide	The serum concentration of Avapritinib can be decreased when it is combined with Enzalutamide.
Epinephrine	The metabolism of Avapritinib can be decreased when combined with Epinephrine.
Erdafitinib	The metabolism of Erdafitinib can be decreased when combined with Avapritinib.
Ergotamine	The metabolism of Avapritinib can be decreased when combined with Ergotamine.
Erythromycin	The metabolism of Avapritinib can be decreased when combined with Erythromycin.
Esketamine	The metabolism of Esketamine can be decreased when combined with Avapritinib.
Estradiol	The metabolism of Estradiol can be decreased when combined with Avapritinib.
Estradiol acetate	The metabolism of Estradiol acetate can be decreased when combined with Avapritinib.
Estradiol benzoate	The metabolism of Estradiol benzoate can be decreased when combined with Avapritinib.
Estradiol cypionate	The metabolism of Estradiol cypionate can be decreased when combined with Avapritinib.
Estradiol dienanthate	The metabolism of Estradiol dienanthate can be decreased when combined with Avapritinib.
Estradiol valerate	The metabolism of Estradiol valerate can be decreased when combined with Avapritinib.
Estrone sulfate	The metabolism of Avapritinib can be decreased when combined with Estrone sulfate.
Etanercept	The metabolism of Avapritinib can be increased when combined with Etanercept.
Ethambutol	The metabolism of Avapritinib can be decreased when combined with Ethambutol.
Ethanol	The metabolism of Avapritinib can be decreased when combined with Ethanol.
Ethinylestradiol	The metabolism of Ethinylestradiol can be decreased when combined with Avapritinib.
Etodolac	The metabolism of Etodolac can be decreased when combined with Avapritinib.
Etoricoxib	The metabolism of Avapritinib can be decreased when combined with Etoricoxib.
Etravirine	The metabolism of Avapritinib can be decreased when combined with Etravirine.
Felbamate	The metabolism of Avapritinib can be decreased when combined with Felbamate.
Felodipine	The metabolism of Avapritinib can be decreased when combined with Felodipine.
Fenofibrate	The metabolism of Avapritinib can be decreased when combined with Fenofibrate.
Flecainide	The metabolism of Avapritinib can be decreased when combined with Flecainide.
Floxuridine	The metabolism of Avapritinib can be decreased when combined with Floxuridine.
Fluconazole	The metabolism of Avapritinib can be decreased when combined with Fluconazole.
Fluindione	The metabolism of Fluindione can be decreased when combined with Avapritinib.
Flunarizine	The metabolism of Flunarizine can be decreased when combined with Avapritinib.
Flunitrazepam	The metabolism of Flunitrazepam can be decreased when combined with Avapritinib.
Fluorouracil	The metabolism of Avapritinib can be decreased when combined with Fluorouracil.
Fluoxetine	The metabolism of Avapritinib can be decreased when combined with Fluoxetine.
Flurbiprofen	The metabolism of Flurbiprofen can be decreased when combined with Avapritinib.
Fluvastatin	The metabolism of Avapritinib can be decreased when combined with Fluvastatin.
Fluvoxamine	The metabolism of Avapritinib can be decreased when combined with Fluvoxamine.
Follitropin	The therapeutic efficacy of Follitropin can be decreased when used in combination with Avapritinib.
Formoterol	The metabolism of Formoterol can be decreased when combined with Avapritinib.
Fosnetupitant	The metabolism of Avapritinib can be decreased when combined with Fosnetupitant.
Fosphenytoin	The metabolism of Fosphenytoin can be decreased when combined with Avapritinib.
Fusidic acid	The metabolism of Avapritinib can be decreased when combined with Fusidic acid.
Gemfibrozil	The metabolism of Avapritinib can be decreased when combined with Gemfibrozil.
Ginkgo biloba	The metabolism of Avapritinib can be decreased when combined with Ginkgo biloba.
Gliclazide	The metabolism of Gliclazide can be decreased when combined with Avapritinib.
Glimepiride	The metabolism of Glimepiride can be decreased when combined with Avapritinib.
Glipizide	The metabolism of Glipizide can be decreased when combined with Avapritinib.
Gliquidone	The metabolism of Gliquidone can be decreased when combined with Avapritinib.
Glyburide	The metabolism of Avapritinib can be decreased when combined with Glyburide.
Golimumab	The metabolism of Avapritinib can be increased when combined with Golimumab.
Haloperidol	The serum concentration of Haloperidol can be increased when it is combined with Avapritinib.
Halothane	The metabolism of Halothane can be decreased when combined with Avapritinib.
Hydromorphone	The metabolism of Hydromorphone can be decreased when combined with Avapritinib.
Ibuprofen	The metabolism of Ibuprofen can be decreased when combined with Avapritinib.
Idarubicin	The metabolism of Idarubicin can be decreased when combined with Avapritinib.
Ifosfamide	The metabolism of Ifosfamide can be decreased when combined with Avapritinib.
Imatinib	The metabolism of Avapritinib can be decreased when combined with Imatinib.
Indinavir	The metabolism of Avapritinib can be decreased when combined with Indinavir.
Indomethacin	The metabolism of Indomethacin can be decreased when combined with Avapritinib.
Infliximab	The metabolism of Avapritinib can be increased when combined with Infliximab.
Irbesartan	The metabolism of Irbesartan can be decreased when combined with Avapritinib.
Isavuconazole	The metabolism of Avapritinib can be decreased when combined with Isavuconazole.
Isavuconazonium	The metabolism of Avapritinib can be decreased when combined with Isavuconazonium.
Isoniazid	The metabolism of Avapritinib can be decreased when combined with Isoniazid.
Isradipine	The metabolism of Avapritinib can be decreased when combined with Isradipine.
Istradefylline	The metabolism of Istradefylline can be decreased when combined with Avapritinib.
Itraconazole	The metabolism of Avapritinib can be decreased when combined with Itraconazole.
Ivosidenib	The metabolism of Avapritinib can be increased when combined with Ivosidenib.
Ketamine	The metabolism of Ketamine can be decreased when combined with Avapritinib.
Ketoconazole	The metabolism of Avapritinib can be decreased when combined with Ketoconazole.
Ketorolac	The metabolism of Ketorolac can be decreased when combined with Avapritinib.
Lacosamide	The metabolism of Lacosamide can be decreased when combined with Avapritinib.
Lansoprazole	The metabolism of Lansoprazole can be decreased when combined with Avapritinib.
Leflunomide	The metabolism of Avapritinib can be decreased when combined with Leflunomide.
Lesinurad	The metabolism of Lesinurad can be decreased when combined with Avapritinib.
Levoketoconazole	The metabolism of Avapritinib can be decreased when combined with Levoketoconazole.
Levothyroxine	The therapeutic efficacy of Levothyroxine can be decreased when used in combination with Avapritinib.
Linagliptin	The metabolism of Avapritinib can be decreased when combined with Linagliptin.
Liothyronine	The therapeutic efficacy of Liothyronine can be decreased when used in combination with Avapritinib.
Liotrix	The therapeutic efficacy of Liotrix can be decreased when used in combination with Avapritinib.
Lonafarnib	The serum concentration of Lonafarnib can be increased when it is combined with Avapritinib.
Lopinavir	The metabolism of Avapritinib can be decreased when combined with Lopinavir.
Lornoxicam	The metabolism of Lornoxicam can be decreased when combined with Avapritinib.
Losartan	The metabolism of Losartan can be decreased when combined with Avapritinib.
Lovastatin	The metabolism of Avapritinib can be decreased when combined with Lovastatin.
Lumacaftor	The metabolism of Avapritinib can be increased when combined with Lumacaftor.
Lumiracoxib	The metabolism of Lumiracoxib can be decreased when combined with Avapritinib.
Lynestrenol	The metabolism of Lynestrenol can be decreased when combined with Avapritinib.
Manidipine	The metabolism of Avapritinib can be decreased when combined with Manidipine.
Mavacamten	The serum concentration of Avapritinib can be decreased when it is combined with Mavacamten.
Medroxyprogesterone	The metabolism of Avapritinib can be decreased when combined with Medroxyprogesterone acetate.
Mefenamic acid	The metabolism of Mefenamic acid can be decreased when combined with Avapritinib.
Meloxicam	The metabolism of Meloxicam can be decreased when combined with Avapritinib.
Mephenytoin	The metabolism of Mephenytoin can be decreased when combined with Avapritinib.
Mestranol	The metabolism of Mestranol can be decreased when combined with Avapritinib.
Methadone	The metabolism of Methadone can be decreased when combined with Avapritinib.
Methimazole	The metabolism of Avapritinib can be decreased when combined with Methimazole.
Methoxyflurane	The metabolism of Methoxyflurane can be decreased when combined with Avapritinib.
Methylene blue	The metabolism of Avapritinib can be decreased when combined with Methylene blue.

Metreleptin	The metabolism of Avapritinib can be increased when combined with Metreleptin.
Metronidazole	The metabolism of Avapritinib can be decreased when combined with Metronidazole.
Miconazole	The metabolism of Avapritinib can be decreased when combined with Miconazole.
Midostaurin	The metabolism of Avapritinib can be decreased when combined with Midostaurin.
Mifepristone	The metabolism of Avapritinib can be decreased when combined with Mifepristone.
Milnacipran	The metabolism of Avapritinib can be decreased when combined with Milnacipran.
Mitotane	The metabolism of Avapritinib can be increased when combined with Mitotane.
Modafinil	The metabolism of Avapritinib can be decreased when combined with Modafinil.
Montelukast	The metabolism of Montelukast can be decreased when combined with Avapritinib.
Nabilone	The metabolism of Nabilone can be decreased when combined with Avapritinib.
Nabumetone	The metabolism of Nabumetone can be decreased when combined with Avapritinib.
Naloxone	The metabolism of Avapritinib can be decreased when combined with Naloxone.
Naproxen	The metabolism of Naproxen can be decreased when combined with Avapritinib.
Nateglinide	The metabolism of Nateglinide can be decreased when combined with Avapritinib.
Nefazodone	The metabolism of Avapritinib can be decreased when combined with Nefazodone.
Nelfinavir	The metabolism of Avapritinib can be decreased when combined with Nelfinavir.
Netupitant	The metabolism of Avapritinib can be decreased when combined with Netupitant.
Nevirapine	The metabolism of Nevirapine can be decreased when combined with Avapritinib.
Nicardipine	The metabolism of Avapritinib can be decreased when combined with Nicardipine.
Niclosamide	The metabolism of Niclosamide can be decreased when combined with Avapritinib.
Nilotinib	The metabolism of Avapritinib can be decreased when combined with Nilotinib.
Nilutamide	The metabolism of Avapritinib can be decreased when combined with Nilutamide.
Nilvadipine	The metabolism of Avapritinib can be decreased when combined with Nilvadipine.
Norgestimate	The metabolism of Norgestimate can be decreased when combined with Avapritinib.
Noscapine	The metabolism of Avapritinib can be decreased when combined with Noscapine.
Olanzapine	The metabolism of Avapritinib can be decreased when combined with Olanzapine.
Olodaterol	The metabolism of Olodaterol can be decreased when combined with Avapritinib.
Omeprazole	The metabolism of Omeprazole can be decreased when combined with Avapritinib.
Ondansetron	The metabolism of Ondansetron can be decreased when combined with Avapritinib.
Oritavancin	The metabolism of Avapritinib can be decreased when combined with Oritavancin.
Ospemifene	The metabolism of Ospemifene can be decreased when combined with Avapritinib.
Oxandrolone	The metabolism of Avapritinib can be decreased when combined with Oxandrolone.
Paramethadione	The metabolism of Paramethadione can be decreased when combined with Avapritinib.
Parathyroid hormone	The therapeutic efficacy of Parathyroid hormone can be decreased when used in combination with Avapritinib.
Parecoxib	The metabolism of Parecoxib can be decreased when combined with Avapritinib.
Paroxetine	The metabolism of Avapritinib can be decreased when combined with Paroxetine.
Peginterferon alfa-2b	The metabolism of Avapritinib can be increased when combined with Peginterferon alfa-2b.
Pentobarbital	The metabolism of Avapritinib can be increased when combined with Pentobarbital.
Phenobarbital	The metabolism of Phenobarbital can be decreased when combined with Avapritinib.
Phenprocoumon	The metabolism of Phenprocoumon can be decreased when combined with Avapritinib.
Phenylbutazone	The metabolism of Avapritinib can be decreased when combined with Phenylbutazone.
Phenytoin	The metabolism of Phenytoin can be decreased when combined with Avapritinib.
Piperaquine	The metabolism of Piperaquine can be decreased when combined with Avapritinib.
Pirfenidone	The metabolism of Pirfenidone can be decreased when combined with Avapritinib.
Piroxicam	The metabolism of Piroxicam can be decreased when combined with Avapritinib.
Pitavastatin	The metabolism of Pitavastatin can be decreased when combined with Avapritinib.
Pitolisant	The serum concentration of Avapritinib can be decreased when it is combined with Pitolisant.
Posaconazole	The metabolism of Avapritinib can be decreased when combined with Posaconazole.
Potassium Iodide	The therapeutic efficacy of Potassium Iodide can be decreased when used in combination with Avapritinib.
Potassium perchlorate	The therapeutic efficacy of Potassium perchlorate can be decreased when used in combination with Avapritinib.
Pralsetinib	The metabolism of Avapritinib can be decreased when combined with Pralsetinib.
Prasugrel	The metabolism of Prasugrel can be decreased when combined with Avapritinib.
Primaquine	The metabolism of Avapritinib can be decreased when combined with Primaquine.
Primidone	The metabolism of Avapritinib can be increased when combined with Primidone.
Probenecid	The metabolism of Avapritinib can be decreased when combined with Probenecid.
Progesterone	The metabolism of Avapritinib can be decreased when combined with Progesterone.
Proguanil	The metabolism of Proguanil can be decreased when combined with Avapritinib.
Promazine	The metabolism of Promazine can be decreased when combined with Avapritinib.
Promethazine	The metabolism of Avapritinib can be decreased when combined with Promethazine.
Propofol	The metabolism of Propofol can be decreased when combined with Avapritinib.
Propylthiouracil	The therapeutic efficacy of Propylthiouracil can be decreased when used in combination with Avapritinib.
Protirelin	The therapeutic efficacy of Protirelin can be decreased when used in combination with Avapritinib.
Quazepam	The metabolism of Quazepam can be decreased when combined with Avapritinib.
Quinidine	The metabolism of Avapritinib can be decreased when combined with Quinidine.
Quinine	The metabolism of Quinine can be decreased when combined with Avapritinib.
Ramelteon	The metabolism of Ramelteon can be decreased when combined with Avapritinib.
Regorafenib	The metabolism of Avapritinib can be decreased when combined with Regorafenib.
Ribociclib	The metabolism of Avapritinib can be decreased when combined with Ribociclib.
Rifampicin	The metabolism of Avapritinib can be increased when combined with Rifampicin.
Rifamycin	The metabolism of Avapritinib can be increased when combined with Rifamycin.
Rifapentine	The metabolism of Avapritinib can be increased when combined with Rifapentine.
Rilonacept	The metabolism of Avapritinib can be increased when combined with Rilonacept.
Rilpivirine	The metabolism of Avapritinib can be decreased when combined with Rilpivirine.
Ritonavir	The serum concentration of Avapritinib can be increased when it is combined with Ritonavir.
Rofecoxib	The metabolism of Rofecoxib can be decreased when combined with Avapritinib.
Rosiglitazone	The metabolism of Rosiglitazone can be decreased when combined with Avapritinib.
Rosuvastatin	The metabolism of Rosuvastatin can be decreased when combined with Avapritinib.
Rucaparib	The metabolism of Avapritinib can be decreased when combined with Rucaparib.
Rupatadine	The metabolism of Rupatadine can be decreased when combined with Avapritinib.
Ruxolitinib	The metabolism of Ruxolitinib can be decreased when combined with Avapritinib.
Salicylic acid	The metabolism of Salicylic acid can be decreased when combined with Avapritinib.
Salmon calcitonin	The therapeutic efficacy of Salmon calcitonin can be decreased when used in combination with Avapritinib.
Saquinavir	The metabolism of Avapritinib can be decreased when combined with Saquinavir.
Satralizumab	The serum concentration of Avapritinib can be decreased when it is combined with Satralizumab.
Secukinumab	The metabolism of Avapritinib can be increased when combined with Secukinumab.
Selegiline	The metabolism of Selegiline can be decreased when combined with Avapritinib.
Selumetinib	The metabolism of Selumetinib can be decreased when combined with Avapritinib.
Sertraline	The metabolism of Avapritinib can be decreased when combined with Sertraline.
Sildenafil	The metabolism of Sildenafil can be decreased when combined with Avapritinib.
Siltuximab	The metabolism of Avapritinib can be increased when combined with Siltuximab.
Simeprevir	The metabolism of Avapritinib can be decreased when combined with Simeprevir.
Simvastatin	The metabolism of Avapritinib can be decreased when combined with Simvastatin.
Siponimod	The metabolism of Siponimod can be decreased when combined with Avapritinib.
Sitaxentan	The metabolism of Avapritinib can be decreased when combined with Sitaxentan.
Somatrogon	The metabolism of Avapritinib can be increased when combined with Somatrogon.
Sorafenib	The metabolism of Avapritinib can be decreased when combined with Sorafenib.
Sotorasib	The serum concentration of Avapritinib can be decreased when it is combined with Sotorasib.
St. John’s Wort	The metabolism of Avapritinib can be increased when combined with St. John’s Wort.
Stiripentol	The metabolism of Avapritinib can be decreased when combined with Stiripentol.
Sulfadiazine	The metabolism of Avapritinib can be decreased when combined with Sulfadiazine.

Sulfamethizole	The metabolism of Avapritinib can be decreased when combined with Sulfamethizole.
Sulfamethoxazole	The metabolism of Avapritinib can be decreased when combined with Sulfamethoxazole.
Sulfaphenazole	The metabolism of Avapritinib can be decreased when combined with Sulfaphenazole.
Sulfapyridine	The metabolism of Avapritinib can be decreased when combined with Sulfapyridine.
Sulfinpyrazone	The metabolism of Avapritinib can be decreased when combined with Sulfinpyrazone.
Sulfisoxazole	The metabolism of Avapritinib can be decreased when combined with Sulfisoxazole.
Tamoxifen	The metabolism of Tamoxifen can be decreased when combined with Avapritinib.
Telaprevir	The metabolism of Avapritinib can be decreased when combined with Telaprevir.
Telithromycin	The metabolism of Avapritinib can be decreased when combined with Telithromycin.
Telotristat ethyl	The serum concentration of Avapritinib can be decreased when it is combined with Telotristat ethyl.
Teniposide	The metabolism of Avapritinib can be decreased when combined with Teniposide.
Tenoxicam	The metabolism of Tenoxicam can be decreased when combined with Avapritinib.
Tepotinib	The metabolism of Avapritinib can be decreased when combined with Tepotinib.
Terbinafine	The metabolism of Terbinafine can be decreased when combined with Avapritinib.
Terfenadine	The metabolism of Avapritinib can be decreased when combined with Terfenadine.
Teriparatide	The therapeutic efficacy of Teriparatide can be decreased when used in combination with Avapritinib.
Testosterone	The metabolism of Testosterone can be decreased when combined with Avapritinib.
Testosterone cypionate	The metabolism of Testosterone cypionate can be decreased when combined with Avapritinib.
Testosterone enanthate	The metabolism of Testosterone enanthate can be decreased when combined with Avapritinib.
Thalidomide	The metabolism of Thalidomide can be decreased when combined with Avapritinib.
Thiamylal	The metabolism of Thiamylal can be decreased when combined with Avapritinib.
Thyroid, porcine	The therapeutic efficacy of Thyroid, porcine can be decreased when used in combination with Avapritinib.
Thyrotropin alfa	The therapeutic efficacy of Thyrotropin alfa can be decreased when used in combination with Avapritinib.
Ticagrelor	The metabolism of Avapritinib can be decreased when combined with Ticagrelor.
Ticlopidine	The metabolism of Avapritinib can be decreased when combined with Ticlopidine.
Tipranavir	The metabolism of Avapritinib can be decreased when combined with Tipranavir.
Tocilizumab	The metabolism of Avapritinib can be increased when combined with Tocilizumab.
Tolazamide	The metabolism of Tolazamide can be decreased when combined with Avapritinib.
Tolbutamide	The metabolism of Tolbutamide can be decreased when combined with Avapritinib.
Tolterodine	The metabolism of Tolterodine can be decreased when combined with Avapritinib.
Torasemide	The metabolism of Avapritinib can be decreased when combined with Torasemide.
Trabectedin	The metabolism of Trabectedin can be decreased when combined with Avapritinib.
Tranylcypromine	The metabolism of Avapritinib can be decreased when combined with Tranylcypromine.
Treprostinil	The metabolism of Treprostinil can be decreased when combined with Avapritinib.
Tretinoin	The metabolism of Tretinoin can be decreased when combined with Avapritinib.
Triclabendazole	The metabolism of Avapritinib can be decreased when combined with Triclabendazole.
Trimethadione	The metabolism of Trimethadione can be decreased when combined with Avapritinib.
Trimethoprim	The metabolism of Trimethoprim can be decreased when combined with Avapritinib.
Trimipramine	The metabolism of Trimipramine can be decreased when combined with Avapritinib.
Troglitazone	The metabolism of Avapritinib can be decreased when combined with Troglitazone.
Troleandomycin	The metabolism of Avapritinib can be decreased when combined with Troleandomycin.
Tucatinib	The metabolism of Tucatinib can be decreased when combined with Avapritinib.
Valdecoxib	The metabolism of Valdecoxib can be decreased when combined with Avapritinib.
Valproic acid	The metabolism of Avapritinib can be decreased when combined with Valproic acid.
Valsartan	The metabolism of Avapritinib can be decreased when combined with Valsartan.
Vemurafenib	The metabolism of Avapritinib can be decreased when combined with Vemurafenib.
Venetoclax	The metabolism of Avapritinib can be decreased when combined with Venetoclax.
Verapamil	The metabolism of Avapritinib can be decreased when combined with Verapamil.
Viloxazine	The metabolism of Avapritinib can be decreased when combined with Viloxazine.
Vismodegib	The metabolism of Vismodegib can be decreased when combined with Avapritinib.
Voriconazole	The metabolism of Avapritinib can be decreased when combined with Voriconazole.
Vortioxetine	The metabolism of Vortioxetine can be decreased when combined with Avapritinib.
Voxelotor	The metabolism of Voxelotor can be decreased when combined with Avapritinib.
Warfarin	The metabolism of Warfarin can be decreased when combined with Avapritinib.
Ximelagatran	The metabolism of Ximelagatran can be decreased when combined with Avapritinib.
Zafirlukast	The metabolism of Avapritinib can be decreased when combined with Zafirlukast.
Zidovudine	The metabolism of Zidovudine can be decreased when combined with Avapritinib.
Zileuton	The metabolism of Zileuton can be decreased when combined with Avapritinib.
Zimelidine	The metabolism of Avapritinib can be decreased when combined with Zimelidine.
Ziprasidone	The metabolism of Avapritinib can be decreased when combined with Ziprasidone.
Zolpidem	The metabolism of Zolpidem can be decreased when combined with Avapritinib.
Zopiclone	The metabolism of Zopiclone can be decreased when combined with Avapritinib.

Pregnanct and Lactations

US FDA pregnancy category: Not assigned

Pregnancy

Based on findings from animal studies and its mechanism of action, AYVAKIT can cause fetal harm when administered to a pregnant woman. There are no available data on AYVAKIT use in pregnant women. Oral administration of avapritinib to pregnant animals during the period of organogenesis was teratogenic and embryotoxic in rats at exposure levels approximately 6.3 and 2.7 times the human exposure based on AUC at the 200 mg and 300 mg dose, respectively. Advise pregnant women of the potential risk to a fetus.

Lactation

Advise women not to breastfeed during treatment with AYVAKIT and for 2 weeks following the final dose

How should this medicine be used?

Avapritinib comes as a tablet to take by mouth. It is usually taken once daily on an empty stomach, at least 1 hour before and 2 hours after a meal. Take avapritinib at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take avapritinib exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

If you vomit after taking avapritinib, do not take another dose. Continue your regular dosing schedule.

Your doctor may decrease your avapritinib dose or stop your treatment depending on how well the medication works for you and if you experience any side effects. Be sure to tell your doctor how you are feeling during your treatment with avapritinib. Do not stop taking avapritinib without talking to your doctor.

Ask your pharmacist or doctor for a copy of the manufacturer’s information for the patient.

What special precautions should I follow?

Before taking avapritinib,

tell your doctor and pharmacist if you are allergic to avapritinib, any other medications, or any of the ingredients in avapritinib tablets. Ask your pharmacist for a list of the ingredients.
tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, and nutritional supplements you are taking or plan to take. Be sure to mention the following: aprepitant (Emend); certain antifungal medications such as fluconazole (Diflucan), itraconazole (Onmel, Sporanox), or ketoconazole; clarithromycin (Biaxin, in Prevpac); diltiazem (Cardizem, Tiazac, others); erythromycin (E.E.S., Erythrocin, others); certain HIV medications such as efavirenz (Sustiva, in Atripla), indinavir (Crixivan), nelfinavir (Viracept), nevirapine (Viramune), ritonavir (Norvir, in Kaletra, others), or saquinavir (Invirase); modafinil (Provigil); nefazodone; oxcarbazepine (Trileptal); phenobarbital; phenytoin (Dilantin, Phenytek); pioglitazone (Actos, in Actoplus, Duetact, Oseni); rifabutin (Mycobutin); rifampin (Rifadin, Rimactane, in Rifater); and verapamil (Calan). Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Many other medications may also interact with avapritinib, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
tell your doctor what herbal products you are taking, especially St. John’s wort.
tell your doctor if you have or have ever had bleeding in your brain, a low platelet (a type of blood cell) counts, or liver or kidney disease. Also, tell your doctor if you have or have ever had a stroke, especially if it has happened within the past year.
tell your doctor if you are pregnant, plan to become pregnant, or if you plan on fathering a child. If you are female, you will need to take a pregnancy test before you start treatment and use birth control to prevent pregnancy during your treatment and for 6 weeks after your final dose. If you are a male, you and your partner should use birth control during your treatment and for 6 weeks after your final dose. Talk to your doctor about birth control methods that you can use during your treatment. If you or your partner become pregnant while taking avapritinib, call your doctor immediately. Avapritinib may harm the fetus.
tell your doctor if you are breast-feeding. You should not breast-feed while you are taking avapritinib and for at least 2 weeks after your final dose.
you should know that this medication may decrease fertility in men and women. Talk to your doctor about the risks of taking avapritinib.
you should know that avapritinib may make you dizzy, drowsy, or confused. Do not drive a car or operate machinery until you know how this medication affects you.

References