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MPharm3 SL32113 > Drugs > Flashcards

Drugs Flashcards

(45 cards)

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1
Q

What are alkylating agents?

A

Alkylating agents are chemotherapy drugs that add alkyl groups to DNA molecules in cancer cells.

Bind covalently to DNA, usually at guanine N7

Causes cross-linking, preventing DNA replication and transcription.

Therefore, the cancer cell cannot divide or survive, leading to cell death.

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2
Q

Cyclophosphamide

A

Alkylating agent (nitrogen mustard)
A prodrug that adds alkyl to DNA
Lymphoma and breast cancer → Haemorrhagic cystitis, myelosuppression

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3
Q

Temozolomide

A

Alkylating agent (triazine)
Methylates DNA at 6 guanine
Glioblastoma → myelosuppression, pneumocystis pneumonia

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4
Q

What are antimetabolites?

A

Drugs that mimic nucleotides, but when incorporated into cells, they disrupt DNA/RNA synthesis and function.

They interfere with nucleotide metabolism by:
- Inhibiting enzymes involved in nucleotide synthesis.
- Incorporating into DNA/RNA in place of normal nucleotides, causing faulty or incomplete strands.

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5
Q

Methotrexate

A

Antimetabolite (folate analogue)
Inhibits dihydrofolate reductase (DHFR) → blocks folate recycling → stops DNA, RNA, and protein synthesis
Leukaemias, Lymphomas → myelosuppression, Mucositis

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6
Q

Pemetrexed

A

Antimetabolite (folate analogue)
Inhibits multiple folate-dependent enzymes: TS, DHFR, blocking DNA synthesis
NSCLC → fatigue, N+V, myelosuppression

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7
Q

5-FU

A

Antimetabolite (pyrimidine analogue)
Inhibits thymidylate synthase (TS) → blocks synthesis of thymidine → stops DNA replication
Gets incorporated into RNA, disrupting RNA processing and function
Colorectal, gastric, panreatic → mucositis, diarrhoea, myelosuppression

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8
Q

FdUMP

A

Active metabolite of 5-Fluorouracil (5-FU)
Forms complex with TS and CH2THF and inhibits TS and blocks synthesis of dTMP

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9
Q

Azacytidine

A

Antimetabolite (pyrimidine analogue + DNMTi)
Gets incorporated into RNA, disrupting function and protein synthesis.
When in DNA, it binds irreversibly to DNMTs) → inhibits DNA methylation, reactivating TSGs and causes apoptosis
Myelodysplastic syndromes, acute myeloid leukaemia → myelosuppression, N+V

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10
Q

Decitabine

A

Antimetabolite (pyrimidine analogue + DNMTi)
Targets DNA only, irreversibly binding to DNMT
Myelodysplastic syndromes, acute myeloid leukaemia → myelosuppression, N+V (better than azacytidine)

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11
Q

6-Thioguanine

A

Antimetabolite (purine analogue)
Converted to 6-thioguanine nucleotides which incorporate into DNA/RNA leading to apoptosis
Acute lymphblastic leukaemia → myelosuppression, GI upset

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12
Q

Cytarabine (Ara-C)

A

Antimetabolite (pyrimidine analogue + sugar-modified nucleoside)
Phosphorylated into ara-CTP, incorporated into DNA, causing chain termination and inhibits DNA polymerase
Acute myeloid/lymphoblastic leukaemias → myelosuppression, N+V

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13
Q

Gemcitabine

A

Antimetabolite (pyrimidine analogue + sugar-modified nucleoside)
Converted to dFdCTP, incorporated into DNA, causes masked chain termination, and inhibits RNR, reducing pool of deoxynucleotides
Pancreatic + NSCLC → myelosuppression, flu-like symptoms

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14
Q

Fludarabine

A

Antimetabolite (pyrimidine analogue + sugar-modified nucleoside)
Converted to active triphosphate form, inhibits DNA polymerase, RNR, and DNA primase, gets incorporated into DNA → causes chain termination → triggers apoptosis
Chronic lymphocytic leukaemia → myelosuppression, immunosuppression

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15
Q

What are antimicrotubule agents?

A

They are drugs that target microtubules—structures inside cells made of tubulin proteins that are essential for:
- Cell shape
- Intracellular transport
- Cell division (mitosis)
Disrupt microtubule dynamics by either:
- Stabilizing microtubules (preventing their disassembly)
- Preventing microtubule formation (polymerization).

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16
Q

Paclitaxel

A

Anti-microtubule (taxane)
Stabilizes microtubules by binding to the β-tubulin subunit, prevents microtubule disassembly, which halts mitosis in M phase of cycle
Breast, ovarian, NSCLC → peripheral neuropathy, myelosuppression

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17
Q

Vincristine

A

Anti-microtubule (vinca alkaloid)
Binds to tubulin, inhibiting microtubule polymerization, prevents microtubule assembly → apoptosis
Acute lymphblastic leukaemia → peripheral neuropathy
(vinblastine is identical except for myelosuppression instead)
(vinorelbine is identical but treats NSCLC instead)

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18
Q

Laulimalide and Peloruside

A

Antimitotic agent (microtubule stabilising agent)
Different binding site to taxanes

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19
Q

Erubulin

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A

Antimitotic agent (microtubule dynamics inhibitor)
Binds to unique site on +ve end, inhibits microtubule polymerisation
Metstatic BC → Peripheral neuropathy, neutropenia

20
Q

What are anti-cancer antibiotics?

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A

Drugs derived from bacteria that interfere with DNA or RNA function in cancer cells, leading to cell death. Damage the genetic material of cancer cells.

  • Intercalate into DNA: Slide between DNA base pairs, disrupting DNA structure.
  • Inhibit topoisomerase enzymes: Blocking the enzymes that unwind DNA during replication to break replication.
  • Generate free radicals: Some produce reactive oxygen species (ROS) that damage DNA and cell membranes
21
Q

Doxorubicin

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A

Anticancer antibiotic (anthracycline)
DNA intercalation – slips between DNA base pairs → disrupts DNA/RNA synthesis
Topoisomerase II inhibition – prevents re-ligation of DNA strands → double-strand breaks
Free radical formation – generates ROS → oxidative damage to DNA, membranes, and proteins
Breast, lymphomas → Cardiotoxicity, myelosuppression, red urine

22
Q

Bleomycins

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A

Anticancer antibiotic
Binds DNA and induces free radical formation in the presence of iron and oxygen, causes single- and double-strand DNA breaks, cell cycle arrest mainly at the G2 phase and apoptosis
Hodgkin’s lymphoma, testicular cancer → pulmonary + skin toxicity

23
Q

Mitomycin C

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A

Anticancer antibiotic (Streptomyces caespitosus) - acts like alkylating agent
Activated inside cells to alkylate and cross-link DNA → stopping replication and triggering apoptosis.
GI and bladder cancer → myelosuppression, pulmonary toxicity

24
Q

Pluramycin

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A

Anti-tumor anthraquinone antibiotic that binds peripherally to the TATA-binding protein (TBP), enhancing alkylation ability
- It functions as a DNA intercalator + minor groove binder and preferentially binds to G-C rich regions in DNA.
- Disrupts transcription initiation, especially in genes with TATA-box–driven promoters or GC-rich sequences nearby.

25
Etoposide
Topoisomerase II inhibitor The enzyme that unwinds DNA during replication and transcription, by stabilizing the DNA–Topoisomerase II complex, re-ligation of DNA strands prevented → causes double-strand breaks → cell cycle arrest Testicular, SCLC → myelosuppression
26
Platins
Act like alkylating agents Forms DNA crosslinks (intra/inter-strand) → apoptosis Cisplatin active immediately, carboplatin is a prodrug Cisplatin: testicular, ovarian, bladder, lung → nephrotoxicity Carboplatin: ovarian, lung, lymphoma → myelosuppression
27
Trastuzumab
Monoclonal antibody (HER2/neu) Binds to domain IV of HER2 receptor - Blocks downstream signaling (MAPK, PI3K/AKT) - Promotes antibody-dependent cellular cytotoxicity (ADCC) - Inhibits HER2 receptor dimerization Humanized IgG1 for HER2+ BC → Cardiotoxicity
28
Bevacizumab
Monoclonal antibody (VEGFA) Binds VEGF-A → prevents it from activating VEGFR on endothelial cells, inhibits angiogenesis (formation of new blood vessels), starves tumor of oxygen and nutrients Colorectal, NSCLC, renal cell carcinoma → HTN, protein uria
29
Pertuzumab
Monoclonal antibody (HER2/neu) - Binds to extracellular domain II of HER2 - Prevents dimerization of HER2 with other HER family receptors - Enhances ADCC (antibody-dependent cellular cytotoxicity) HER2+ BC → diarrhoea, cardiotoxicity
30
Imatinib
TKI (BCR-ABL) - Binds to ATP-binding site of BCR-ABL → blocks its tyrosine kinase activity - Inhibits abnormal cell proliferation driven by constitutively active BCR-ABL Chronic myeloid leukaemia, acute lymphoblastic leukaemia → oedema, myelosuppression
31
Erlotinib
TKI (EGFR) - Binds to the ATP-binding site of EGFR tyrosine kinase domain - Inhibits downstream signaling pathways (RAS/RAF/MEK, PI3K/AKT) involved in cell proliferation and survival NCSLC, pancreatic → acneform rash, GI upset
32
Crizotinib
TKI (ALK, ROS1) - Inhibits ALK and ROS1 fusion proteins that drive tumor growth - Blocks ATP-binding site, preventing kinase activation and downstream signaling (cell growth and survival) ALK+ or ROS1+ NSCLC → visual disturbance, GI issues, oedema
33
Gefitinib
TKI (EGFR) - Binds reversibly to the ATP-binding site of EGFR tyrosine kinase domain - Blocks downstream signaling pathways (RAS/RAF/MEK, PI3K/AKT) leading to inhibition of tumor cell proliferation and survival NSCLC → Acneform rash, GI upset
34
Ceritinib
TKI (ALK) - Inhibits ALK tyrosine kinase by blocking ATP binding site - Prevents downstream signaling involved in cell growth and survival ALK+ NSCLC → GI upset
35
Lapatinib
TKI (HER2 EGFR) - Reversibly inhibits the intracellular tyrosine kinase domains of HER2 and EGFR - Blocks downstream signaling pathways (MAPK, PI3K/AKT) involved in cell proliferation and survival HER2+ BC → GI upset
36
TDM-1
ADC (HER2) - Combines trastuzumab (HER2 monoclonal antibody) with DM1, a cytotoxic microtubule inhibitor - Trastuzumab binds HER2-positive cancer cells, delivering DM1 directly inside - DM1 disrupts microtubules → cell cycle arrest and apoptosis HER2 metastatic BC → fatigue, nausea
37
Tamoxifen
Selective estrogen receptor modulator (ER) - Acts as an antagonist of ER in breast tissue, blocking estrogen binding - Prevents estrogen-driven proliferation of ER-positive breast cancer cells - Has partial agonist effects in other tissues (e.g., bone, uterus) ER-+ BC, BC prevention in high-risk women → menopausal symptoms
38
Anastrozole
Aromatase inhibitor - Blocks aromatase, the enzyme that converts androgens into estrogens - Lowers estrogen levels, reducing estrogen-driven growth in ER-positive breast cancer Postmenopausal women with ER-+ BC → menopausal symptoms
39
Bicalutamide/Flutamide
Non-steroidal anti-androgen (AR) - Competitively inhibits androgen binding to AR in prostate cancer cells - Blocks androgen-driven growth and survival signals Prostate Cancer → gynecomastia, hot flashes
40
Enzalutamide
2nd gen non-steroidal anti-androgen (AR) - Inhibits androgen binding to AR - Blocks AR nuclear translocation - Prevents AR binding to DNA and co-activator recruitment - Stronger inhibition than first-generation antiandrogens Metastatic castration-resistant prostate cancer (mCRPC) → fatigue, hot flashes
41
Pembrolizumab/Nivolumab
Immune checkpoint inhibitors (Anti-PD-1 mAbs) - Block PD-1 receptor interaction with its ligands (PD-L1/PD-L2) - Reactivate T cells by preventing "immune checkpoint" suppression - Promote immune system attack on cancer cells Melonoma, NSCLC, head & neck, bladder → immune-related adverse events
42
Atezolizumab/Durualumab
Immune checkpoint inhibitors (Anti-PD-L1 mAbs) - Bind to PD-L1, blocking its interaction with PD-1 receptor on T cells - Prevent tumor cells from suppressing T cell activation - Enhance immune-mediated tumor cell killing TNBC, NSCLC → Immune-related adverse events
43
Rucaparib/Niraparib
PARP inhibitor (Poly ADP-ribose polymerase) - Inhibits PARP enzymes, preventing repair of single-strand DNA breaks - Leads to accumulation of DNA damage, especially lethal in cancer cells with BRCA1/2 mutations (defective homologous recombination repair) Rucaparib: BRCA mutated ovarian + prostate cancers → nausea, fatigue, anaemia Niraparib: Maintenance for ovarian + fallopian after platins → thrombocytopenia
44
Etanidazole
Hypoxic cell radiosensitizer - Sensitizes hypoxic tumor cells to radiation therapy by mimicking oxygen - Enhances radiation-induced DNA damage in oxygen-poor (hypoxic) cancer cells which are usually resistant to radiation Neurotoxicity, peripheral neuropathy
45
Ramucirumab
Monoclonal antibody (VEGFR2/angiogenesis inhibitor) - Binds VEGFR-2, blocking VEGF ligands from activating the receptor - Inhibits angiogenesis (formation of new blood vessels) needed for tumor growth and metastasis Gastric, NSCLC, colorectal → HTN, fatigue

MPharm3 SL32113 (5 decks)

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