Anticancer drugs

Question 1

Alkylating agents

Answer 1

MOA: inserts alkyl group, cross-links G bases, DNA breakage, apoptosis

STAGE: all stages

E.G. cyclophosphamides, platinum compounds

Question 2

Cytotoxic antibiotics

Answer 2

MOA: inhibits transcription and translation (e.g., by preventing topoisomerase II action)

STAGE: G1, G2 phase

E.G. doxorubicin

• Metabolised by CYP3A4 hence drug interactions may occur with rifampicin and St John’s wort

Question 3

Antimetabolites

Answer 3

MOA: substitute themselves into DNA synthesis

CYCLE STAGE: S-phase

E.G., Methotrexate, Fluouracil

Question 4

Plant alkaloids: mitotic poisons

Answer 4

MOA: prevent spindle formation

STAGE: M-phase

E.G. vinca alkaloids, taxanes

Question 5

Plant alkaloids: topoisomerase inhbitors

Answer 5

MOA: inhibit topoisomerase, interfere with DNA (un)coiling

STAGE: S/G2 phase

E.G. doxorubicin

Question 6

Hormone antagonists for BREAST CANCER

Answer 6

G1 PHASE

SERM (selective oestrogen receptor modulator)

MOA: binds to oestrogen receptors, “modulator drug” (acts as agonist (bone and ovaries) and antagonist (breast))

E.G. tamoxifen

Aromatase inhibitor

MOA: inhibits androgens –> oestrogen to decrease circulating oestrogen

E.G. anastrozole

Question 7

Hormone antagonists for PROSTATE CANCER

Answer 7

G1 PHASE

Antiandrogens

MOA: inhibits androgens effect

E.G. bicalutamid

Gonadotropin-releasing hormones (GnRH) analogues

MOA: competitive inhibitor of GnRH, prevents sex hormones secretions

Question 8

Hormone antagonists for LYMPHOMAS/LEUKAEMIAS

Answer 8

G1 PHASE

MOA: arrest growth, induce apoptosis in lymphoid tissue

E.G. prednisolone

Question 9

mAbs

Answer 9

• Rituximab: anti-CD20 mAb, triggers B cell lysis, used in non-Hodgkin’s lymphoma
• Trastuzumab: binds to HER2 receptors, used in breast cancer

Question 10

Immunomodulating agents/ biological response modifiers

Answer 10

MOA: improve immune response

E.G. interferons (cytotoxicity), interleukin-2 (proliferation), checkpoint inhibitors (anti-PD1 - prevents T-cell apoptosis, anti-CTLA 4 - prevents T cells from turning off)

Question 11

Protein kinase inhibitors

Answer 11

MOA: inactivate enzymes associated with cell signalling and proliferation, only used for GIT tumors and leukaemia

E.G. suffix: -INIB

TYROSINE KINASE RECEPTOR = PROTO-ONCOGENE

Question 12

Sensitising agents

Answer 12

MOA: makes cells superficial to the tumour more recognisable to the immune system

Question 13

Managing side effects

Answer 13

Analgesics: relieve pain

Antiemetic: reduce nausea and vomiting, e.g. setrons

CSF: stimulate leukocyte production, e.g. filigrastim (stimulates WBCs), erythropoietin (stimulates RBCs)

Question 14

AEs

Answer 14

• aloplecia
• nausea/vomiting
• skin blistering and necrosis
• infertility
• decreased haemopoiesis, anaemia
• paraesthesia
• renal toxicity
• dysrythmia