Anticancer Drug; The latest classification of anti cancer drug

Last updated: February 7, 2026Reviewed date: February 7, 2026Reading time: 7 min read

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Simple patient meaning: Anticancer or antineoplastic drugs are used to treat malignancies, or cancerous growths&control the growth of cancerous cells. Cancer is commonly defined as the uncontrolled growth of cells, with loss of differentiation and commonly, with metastasis, the spread of cancer to other tissues and organs. Cancers are malignant growths. In contrast, benign growths remain encapsulated and grow within a well-defined area. Drug therapy may be used alone or in combination with other treatments such as surgery or radiation therapy. The top 10 best-selling (in terms of revenue) cancer drugs list No. Global Sales INN Trade names Marketing authorization holder Indications 1 $7.78 billion Rituximab Rituxan, MabThera Roche, Pharmstandard non-Hodgkin's lymphoma, CLL 2 $6.75 billion Bevacizumab...

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Anticancer or antineoplastic drugs are used to treat malignancies, or cancerous growths&control the growth of cancerous cells. Cancer is commonly defined as the uncontrolled growth of cells, with loss of differentiation and commonly, with metastasis, the spread of cancer to other tissues and organs. Cancers are malignant growths. In contrast, benign growths remain encapsulated and grow within a well-defined area. Drug therapy may be used alone or in combination with other treatments such as surgery or radiation therapy. The top 10 best-selling (in terms of revenue) cancer drugs list No. Global Sales INN Trade names Marketing authorization holder Indications 1 $7.78 billion Rituximab Rituxan, MabThera Roche, Pharmstandard non-Hodgkin's lymphoma, CLL 2 $6.75 billion Bevacizumab...

For severe symptoms, danger signs, pregnancy, child illness, or sudden worsening, seek urgent medical care.

বাংলা রোগী নোট এখনো যোগ করা হয়নি। পোস্ট এডিটরে “RX Bangla Patient Mode” বক্স থেকে সহজ বাংলা সারাংশ যোগ করুন।

এই তথ্য শিক্ষা ও সচেতনতার জন্য। এটি ডাক্তারি পরীক্ষা, রোগ নির্ণয় বা প্রেসক্রিপশনের বিকল্প নয়।

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This article explains The top 10 best-selling (in terms of revenue) cancer drugs list in simple medical language.
This article explains Newer and experimental approaches in simple medical language.
This article explains Polyfunctional alkylating agents of Anticancer Drug in simple medical language.

Educational health guideWritten for patient understanding and clinical awareness.

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Emergency safety firstUrgent warning signs are highlighted below.

Seek urgent medical care if you notice

These warning signs are general safety guidance. Local emergency numbers and clinical judgment should always come first.

Severe symptoms, breathing difficulty, fainting, confusion, or rapidly worsening illness.
New weakness, severe pain, high fever, or symptoms after a serious injury.
Any symptom that feels urgent, unusual, or unsafe for the patient.

Emergency now

Use emergency care for severe, sudden, rapidly worsening, or life-threatening symptoms.

See a doctor

Book a professional medical evaluation if symptoms persist, worsen, recur often, affect daily activities, or occur in a high-risk patient.

Learn safely

Use this article to understand possible causes, tests, treatment options, prevention, and questions to ask your clinician.

Anticancer or antineoplastic drugs are used to treat malignancies, or cancerous growths&control the growth of cancerous cells. Cancer is commonly defined as the uncontrolled growth of cells, with loss of differentiation and commonly, with metastasis, the spread of cancer to other tissues and organs. Cancers are malignant growths. In contrast, benign growths remain encapsulated and grow within a well-defined area. Drug therapy may be used alone or in combination with other treatments such as surgery or radiation therapy.

The top 10 best-selling (in terms of revenue) cancer drugs list

No.	Global Sales	INN	Trade names	Marketing authorization holder	Indications
1	$7.78 billion	Rituximab	Rituxan, MabThera	Roche, Pharmstandard	non-Hodgkin’s lymphoma, CLL
2	$6.75 billion	Bevacizumab	Avastin	Roche	Colorectal, lung, ovarian and brain cancer
3	$6.56 billion	Trastuzumab	Herceptin	Roche	Breast, esophagus and stomach cancer
4	$4.69 billion	Imatinib	Gleevec	Novartis	Leukemia, GI cancer
5	$1.09 billion	Lenalidomide	Revlimid	Celgene, Pharmstandard	Multiple myeloma, mantle cell lymphoma
6	$2.7 billion	Pemetrexed	Alimta	Eli Lilly	Lung cancer
7	$2.6 billion	Bortezomib	Velcade	Johnson & Johnson, Takeda, Pharmstandard	Multiple myeloma
8	$1.87 billion	Cetuximab	Erbitux	Merck KGaA, Bristol-Myers Squibb	Colon and head and neck cancer
9	$1.73 billion	Leuprorelin	Lupron, Eligard	AbbVie and Takeda; Sanofi and Astellas Pharma	Prostate and ovarian cancer
10	$1.7 billion	Abiraterone	Zytiga	Johnson & Johnson	Prostate cancer

Polyfunctional alkylating agents

Nitrosourea
Mustards (Nitrogen Mustards)
Methanesulphonates (Busulphan)
Ethylenimines

Other Alkylating Drugs

Procarbazine (Matulane)
Dacarbazine (DTIC)
Altretamine (Hexalen)
Cisplatin (Platinol)

Antimetabolites

Antifolic acid compounds (Methotrexate)
Amino acid Antagonists (Azaserine)

Purine antagonists

Mercaptopurine (6-MP)
Thioguanine (6-TG)
Fludarabine Phosphate
Cladribine (Leustatin)
Pentostatin (Nipent)

Pyrimidine antagonists

Mucositis
Fluorouracil (5-FU)
Cytarabine (ARA-C)
Azacitidine

Plant alkaloids

Vinblastine (Velban)
Vincristine (Oncovin)
Etoposide (VP-16,VePe-sid)
Teniposide (Vumon)
Topotecan (Hycamtin)
Irinotecan (Camptosar)
Paclitaxel (Taxol)
Docetaxel (Taxotere)

Antibiotics

Anthracyclines
Doxorubicin (Adriamycin, Rubex, Doxil)
Daunorubicin (DaunoXome)
Dactinomycin (Cosmegen)
Idarubincin (Idamycin)
Plicamycin (Mithramycin)
Mitomycin (Mutamycin)
Bleomycin (Blenoxane)

Monoclonal Antibodies Hormonal agents

Tamoxifen (Nolvadex)
Flutamide (Eulexin)
Gonadotropin-Releasing Hormone Agonists
(Leuprolide and Goserelin (Zoladex))
Aromatase Inhibitors
Aminoglutethimide
Anastrozole (Arimidex)

Miscellaneous anticancer drugs

Amsacrine
Hydroxyurea (Hydrea)
Asparaginase (El-spar)
Mitoxantrone (Novantrone)
Mitotane
Retinoic Acid Derivatives
Bone Marrow Growth Factors
Amifostine

Newer and experimental approaches

Hematopoietic stem cell transplant approaches – Stem cell harvesting and autologous or allogeneic stem cell transplant have been used to allow for higher doses of chemotherapeutic agents where dosages are primarily limited by hematopoietic damage. Years of research in treating solid tumors, particularly breast cancer, with hematopoeitic stem cell transplants, has yielded little proof of efficacy. Hematological malignancies such as myeloma, lymphoma, and leukemia remain the main indications for stem cell transplants.

Isolated infusion approaches – Isolated limb perfusion (often used in melanoma), or isolated infusion of chemotherapy into the liver or the lung have been used to treat some tumors. The main purpose of these approaches is to deliver a very high dose of chemotherapy to tumor sites without causing overwhelming systemic damage. These approaches can help control solitary or limited metastases, but they are by definition not systemic, and, therefore, do not treat distributed metastases or micrometastases.

Targeted delivery mechanisms – Specially-targeted delivery vehicles aim to increase effective levels of chemotherapy for tumor cells while reducing effective levels for other cells. This should result in an increased tumor kill and/or reduced toxicity. Specially-targeted delivery vehicles have a differentially higher affinity for tumor cells by interacting with tumor-specific or tumor-associated antigens.
In addition to their targeting component – they also carry a payload – whether this is a traditional chemotherapeutic agent, or a radioisotope or an immune-stimulating factor. Specially-targeted delivery vehicles vary in their stability, selectivity, and choice of target, but, in essence, they all aim to increase the maximum effective dose that can be delivered to the tumor cells. Reduced systemic toxicity means that they can also be used in sicker patients, and that they can carry new chemotherapeutic agents that would have been far too toxic to deliver via traditional systemic approaches.

Nanoparticles – Nanoparticles have emerged as a useful vehicle for poorly-soluble agents such as paclitaxel. Protein-bound paclitaxel (e.g., Abraxane) or nab-paclitaxel was approved by the U.S. Food and Drug Administration (FDA) in January 2005 for the treatment of refractory breast cancer and allows reduced use of the Cremophor vehicle usually found in paclitaxel. Nanoparticles made of magnetic material can also be used to concentrate agents at tumor sites using an externally applied magnetic field.

Polyfunctional alkylating agents of Anticancer Drug

Common Structural Features

bis(chloroethyl)amine
ethylenimine
nitrosoureas

Not cell-cycle specific – Cells most susceptible in late G1 and S phase– Blocks in G2
Most useful agents

Cyclophosphamide (Cytoxan)
ifosfamide
Mechlorethamine
Melphalan (Alkeran)
Chlorambucil (Leukeran) Secondary agents
Thiopental (Thioplex)
Ovarian cancer
Busulfan (Mylan)
Chronic myeloid leukemia

Major nitrosoureas

Carmustine (BCNU)
Lomustine (CCNU)
Semustine (methyl CCNU)

Polyfunctional Alkylating Drugs

Mechanism of Action: Alkyl group transfer and Major interaction: Alkylation of DNA
Primary DNA alkylation site: N7 position of guanine (other sites as well)
the interaction may involve single strands or both strands (cross-linking, due to bifunctional characteristics)
Other interactions: these drugs react with carboxyl, sulfhydryl, amino, hydroxyl, and phosphate groups of other cellular constituents
These drugs usually form a reactive intermediate ethyleneimonium ion

Polyfunctional Alkylating Drug Resistance

Increased ability to repair DNA defects
Decreased cellular permeability to the drug
Increased glutathione synthesi
inactivates alkylating agents through conjugation reactions (catalyzed by glutathione S-transferase)
Polyfunctional Alkylating Drugs:
Genotoxic carcinogens, able to damage DNA by alkylation reactions, represent a very diverse class of agents which are capable of producing a wide range of DNA modifications. The mechanisms leading to genetic changes as a result of exposure to alkylating agents (AAs) have been studied in male germ cells of Drosophila using a structure-activity relationship approach (SAR).
The analytical tools available concern both genetic and molecular assays. The genetic tests enable to quantify excision repair and clastogenic potency of the AA after treatment of post-meiotic male germ cells and to determine the degree of germ-cell specificity, i.e., the mutagenic effectiveness in the post- versus premeiotic cell stages. For a selected group of alkylating agents, the molecular spectra have been studied in post-meiotic cell stages.
On the basis of these descriptors, clear SAR’s between genotoxic activity in germ cells and physicochemical parameters (s-values and O6/N7-alkylguanine adducts) and carcinogenic potency in rodents became apparent, resulting in five distinct classes of alkylating agents so far.
These classes are: 1) SN2-type monofunctional AAs, 2) SN1-type monofunctional AAs, 3) polyfunctional AAs, 4) agents able to form etheno-DNA adducts, and 5) aflatoxin B1 (AFB1) a bulky-adduct forming agent. The recent finding that the molecular data obtained with Drosophila and data of the specific locus tests in male mice show remarkable similarities for most genotoxic agents supports the view that Drosophila is a useful model system for the study of transgenerational damage.

Pharmacological Effects: Polyfunctional Alkylating Drugs

Injection site damage (vesicant effects) and systemic toxicity.
Toxicity:dose-related primarily affecting rapidly dividing cells bone marrow
GI tract nausea and vomiting within less than an hour– with mechlorethamine, carmustine (BCNU) or cyclophosphamide Emetic effects: CNS reduced by pre-treatment with phenothiazines or cannabinoids.
gonads
Cyclophosphamide cytotoxicity depends on activation by microsomal enzyme system. Hepatic microsomal P450 mixed-function oxidase catalyzes the conversion of cyclophosphamide to the active forms:
hydroxycyclophosphamide aldophosphamide
Major Toxicity: bone marrow suppression dose-related suppression of myelopoiesis: primary effects on megakaryocytes platelets granulocytes. Bone marrow suppression is worse when alkylating agents are combined with other myelosuppressive drugs and/or radiation (dose reduction required)
If bone marrow suppression is severe, treatment may have to be suspended and then re-initiated upon hematopoietic recovery. Long-term consequences of alkylating agent treatment include: ovarian failure (common) testicular failure (common) acute leukemia (rare)

Oral Route of Administration

Cyclophosphamide (Cytoxan), melphalan (Alkeran), chlorambucil (Leukeran), busulfan (Myleran), lomustine (CCNU, CeeNU)

Cyclophosphamide (Cytoxan): most useful alkylating agent at present.
Busulfan (Myleran): specificity for granulocytes — chronic myelogenous leukemia

Nitrosoureas

Not cross-reactive (with respect to tumor resistance) with other alkylating drugs.
Nonenzymatic by transformation required to activate compounds. Highly lipid-soluble– crosses the blood-brain barrier (BBB useful in treating brain tumors
Act by cross-linking: DNA alkylation
More effective against cells in plateau phase than cells in the exponential growth phase
The major route of elimination: urinary excretion of antidiabetic agents.

Other Alkylating Drugs

Procarbazine (Matulane)
Methylhydrazine derivative
Active in Hodgkin’s disease (combination therapy)
Teratogenic, mutagenic, leukemogenic.
Dacarbazine (DTIC)

References

Anticancer Drug; The latest classification of anti cancer drug

Safety note: This is not a prescription or diagnosis. For severe symptoms, pregnancy danger signs, children with serious illness, chest pain, breathing difficulty, stroke-like weakness, or major injury, seek urgent care.

Which doctor may help?

Start with a registered doctor or the nearest qualified health center.

What to tell the doctor

Write when the problem started and how it changed.
Bring old prescriptions, investigation reports, and current medicines.
Write allergies, pregnancy status, diabetes, kidney/liver disease, and major past illnesses.
Bring one family member if the patient is weak, elderly, confused, or a child.

Questions to ask

What is the most likely cause of my symptoms?
Which danger signs mean I should go to hospital quickly?
Which tests are necessary now, and which can wait?
How should I take medicines safely and what side effects should I watch for?
When should I come for follow-up?

Tests to discuss

Vital signs: temperature, pulse, blood pressure, oxygen saturation
Basic physical examination by a clinician
CBC, urine test, blood sugar, or imaging only when clinically needed

Avoid these mistakes

Do not use antibiotics, steroid tablets/injections, or strong painkillers without proper medical advice.
Do not hide pregnancy, kidney disease, ulcer, allergy, or blood thinner use.
Do not delay emergency care when danger signs are present.

Medicine safety and first-aid guide

This section is for patient education only. It does not replace a doctor, pharmacist, or emergency care.

Safe first steps

Rest, drink safe water, and observe symptoms carefully.
Keep a written note of symptoms, duration, temperature, medicines already taken, and allergy history.
Seek medical care quickly if symptoms are severe, worsening, or unusual for the patient.

OTC medicine safety

For mild pain or fever, ask a registered pharmacist or doctor before using common over-the-counter pain/fever medicines.
Do not combine multiple pain medicines without advice, especially if you have kidney disease, liver disease, stomach ulcer, asthma, pregnancy, or take blood thinners.
Do not give adult medicines to children unless a qualified clinician advises it.

Avoid these mistakes

Do not start antibiotics without a proper medical decision.
Do not use steroid tablets or injections casually for quick relief.
Do not delay emergency care because of home remedies.

Get urgent help if

Severe symptoms, confusion, fainting, breathing difficulty, chest pain, severe dehydration, or sudden weakness need urgent medical care.

Medicine names, dose, and timing must be decided by a qualified clinician or pharmacist after checking age, pregnancy, allergy, other diseases, and current medicines.

For rural patients and family caregivers

Patient health record and symptom diary

Write your symptoms, medicines already taken, test results, and questions before visiting a doctor. This note stays on your device unless you print or copy it.

Doctor to discuss: Doctor / qualified healthcare provider

Tests to discuss with doctor

Basic vital signs: temperature, pulse, blood pressure, oxygen level if needed
Relevant blood, urine, imaging, or specialist tests only after clinical assessment

Questions to ask

What is the most likely cause of my symptoms?
Which warning signs mean I should go to emergency care?
Which tests are really needed now?
Which medicines are safe for my age, pregnancy status, allergy, kidney/liver/stomach condition, and current medicines?

Emergency warning signs such as chest pain, severe breathing difficulty, sudden weakness, confusion, severe dehydration, major injury, or loss of bladder/bowel control need urgent medical care. Do not wait for online information.

Go to emergency care if you notice:

Severe or rapidly worsening symptoms
Breathing difficulty, chest pain, fainting, confusion, severe weakness, major injury, or severe dehydration

Doctor / service to discuss: Qualified healthcare provider; specialist depends on symptoms and examination.

Step 1
Check danger signs first
If danger signs are present, seek emergency care and do not wait for online information.
Step 2
Record the symptom story
Write when symptoms started, severity, medicines already taken, allergies, pregnancy status, and test results.
Step 3
Visit a qualified clinician
A doctor, nurse, or qualified healthcare provider can examine you and decide which tests or treatment are needed.
Step 4
Do only useful tests
Do tests after clinical assessment. Avoid unnecessary tests, random antibiotics, or repeated medicines without diagnosis.
Step 5
Follow up and return early if worse
If symptoms worsen, new warning signs appear, or treatment is not helping, return for review quickly.

Rural patient practical tips

Take a written symptom diary and all previous prescriptions/test reports.
Do not hide medicines already taken, even herbal or over-the-counter medicines.
Ask which warning signs mean urgent referral to hospital.

This roadmap is for education. A real diagnosis and treatment plan requires history, examination, and clinical judgment.

RX Patient Help

Ask a health question safely

Write your symptom story. A health professional or site editor can review it before any answer is prepared. This box is not for emergency care.

Emergency first: Severe chest pain, breathing trouble, unconsciousness, stroke signs, severe injury, heavy bleeding, or rapidly worsening symptoms need urgent local medical care now.

Frequently Asked Questions

Is this article a replacement for a doctor?

No. It is educational content only. Patients should consult a qualified clinician for diagnosis and treatment.

When should I seek urgent care?

Seek urgent care for severe symptoms, rapidly worsening condition, breathing difficulty, severe pain, neurological changes, or any emergency warning sign.

References

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Anticancer Drug; The latest classification of anti cancer drug

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