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Pharmacology

Antineoplastic agents

8 topics with a brief review: definitions, key facts, and classroom questions.

This section is dedicated to the pharmacology of antineoplastic agents, one of the most complex and clinically significant topics. Here we examine drugs that inhibit the growth of malignant neoplasms. You will study basic cytostatics: alkylating agents, antimetabolites, antitumor antibiotics, and plant-derived agents, as well as enzymes and topoisomerase inhibitors.

A separate module is devoted to treatment methods with increased selectivity of action. We will take a detailed look at hormonal antineoplastic agents and targeted drugs that precisely block the molecular targets of tumor cells, reducing systemic toxicity.

In seminars and exams, instructors most frequently ask about the sites of drug action in the cell cycle (specifically how DNA synthesis or cell division is disrupted), characteristic side effects (myelosuppression, anthracycline cardiotoxicity), and the principles of combination chemotherapy. A solid understanding of these mechanisms is the foundation for mastering modern oncology.

Section Topics

Frequently asked questions for this section

What is the core principle of the cell cycle synchronization method?

This is a two-step strategy. First, a drug is administered that blocks cells in a single phase (e.g., vincristine in the M phase). Once the surviving cells simultaneously transition to the next stage, a second strike is delivered with a phase-specific agent (e.g., cytarabine in the S phase).

Why is methotrexate inactive against resting cells?

The drug is a strict phase-specific agent. It acts exclusively during the S phase of the cell cycle when active DNA synthesis takes place.

In which phase of the cell cycle do alkylating drugs act?

They are cell cycle-nonspecific. DNA cross-linking occurs in any phase, although actively dividing cells are most sensitive to their effects.

Why are antitumor antibiotics administered exclusively intravenously?

Most drugs in this group, such as anthracyclines and dactinomycin, are completely destroyed by gastrointestinal enzymes or do not cross the gut wall into the bloodstream at therapeutic doses.

In which phase of the cell cycle do vinca alkaloids act?

They are phase-specific agents and act exclusively in the M phase (mitosis), arresting cell division at the metaphase stage.

Why cannot antiandrogens be used as monotherapy?

Receptor blockade by antiandrogens (e.g., flutamide) removes the inhibitory effect of testosterone on gonadotropin secretion. This causes a reflex surge of LH and a new spike in testosterone production, which is why combination with GnRH analogues is required.

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