Anti-Cancer Drugs
Anti-cancer Drugs which do NOT cause Bone Marrow Suppression
Drug | Key Point |
Vincristine | • Disruption of microtubules S/E • Peripheral neuropathy • SIADH |
Asparaginase | Used For ALL S/E • Allergy • Acute Pancreatitis • Blew horns on skin → pigmentation |
Bleomycin | • Causes DNA strand breaks • Marrow sparing S/E • Pulmonary fibrosis • Flagellated pigmentation of skin • Blew horns on skin → pigmentation |
Chlorambucil | ㅤ |
- Christians () blew () with chlorine () and asparagus ()
Anticancer drugs can be divided into
- Cytotoxic
- Targeted
Classification
G₂ phase | ㅤ |
↳ Bleomycin | • Causes DNA strand breaks • Marrow sparing S/E • Pulmonary fibrosis • Flagellated pigmentation of skin • Blew horns on skin → pigmentation |
S Phase | ㅤ |
• Affect Folic Acid Metabolism | ㅤ |
↳ Methotrexate | • ⛔ dihydrofolate reductase enzyme Uses • Choriocarcinoma - D.O.C • Rheumatoid arthritis - D.O.C S/E • Bone marrow suppression ↳ Pemetrexed > Methotrexate Toxicity treatment • Folinic acid (Leucovorin or Citrovorum) + • Vitamin B12 injection for Pemetrexed |
• Affect Purine Metabolism | ㅤ |
↳ Cladribine | • ⛔ ADA (like SCID) • Used in HCL • Antimetabolite + Cell cycle Nonspecific • Clara → hairy |
↳ Fludarabine | • Used in CLL • Flood → Call |
↳ 6 - Mercaptopurine | • Hepatotoxic |
↳ 6 - Thioguanine | • Hepatotoxic |
• Affect Pyrimidine Metabolism | ㅤ |
↳ Cytarabine | • Cause cerebellar side effects • Sit when ataxia (cerebellar s/e) |
↳ 5-Fluorouracil | • Capecitabine (Prodrug) • Hand and foot syndrome ⤿[Capecitabine > 5-Fluorouracil [5-FU] |
↳ Pentostatin | • ⛔ ADA (like SCID) |
↳ Thiopurines | ㅤ |
↳ Gemcitabine | • DOC for Pancreatic carcinoma • Pancreas is a gem |
M Phase | • Win (vincristine, vinblastine) a Packet (Paclitaxel) • by rotating spindle |
Microtubule Inhibitors | ㅤ |
↳ Taxanes | • Hyperstabilization of microtubules • Tax stabilise society |
↳ Paclitaxel | ㅤ |
↳ Vinca alkaloids | • Disruption of microtubules S/E • Peripheral neuropathy • SIADH |
↳ Vincristine | • Marrow sparing • Used in Retinoblastoma, ALL, Langerhans |
↳ Vinblastine | • ABVD regimen for NCHL |
Topoisomerase Inhibitors | Top (Topoisomerase) → Irene (Irenetecan) nte top sidilott (Etoposide) poi → ruby (Donorubi……) kandu |
Topo II | ㅤ |
↳ Etoposide | ㅤ |
↳ Teniposide | ㅤ |
Topo I | ㅤ |
↳ Irinotecan | • Used for colorectal carcinoma • Cholinergic S/E |
↳ Topotecan | ㅤ |
Cell Cycle–Independent Drugs | ㅤ |
Platinum Compounds | ㅤ |
↳ Cisplatin | S/E • Ototoxicity • Nephrotoxicity (⛔ Reabsorption in distal tubules) ↳ Hypokalemia ↳ Hypomagnesemia ↳ Hypocalcemia ↳ Hypophosphatemia • Max Nausea & Vomiting Prevention • 1-2 L NS → Chloride diuresis → inactivate cisplatin • then Mannitol → to throw Cisplatin from body • then Amifostine → to reduce S/E of radiotherapy • Sis nu Plate kodukk → Amikk first (Amfostine) kodukk |
Alkylating Agents | • Cause DNA cross-linking Must (mustine drugs) buy Mighty (mitomycin c,melphalan) Car (Procarbazine) Bus (Busulfan) Cycle (cyclophosp) from Temu () → ↓↓ Price →→ ↓↓ H+ (Temu → alkylating agent) |
↳ Cyclophosphamide (Nitrogen mustards) | S/E • Hemorrhagic cystitis • SIADH • Pulmonary fibrosis • Cycle and Bus → Poka adikkum → Pulm fibrosis Hemorrhagic cystitis • Metabolite responsible is acrolein • Prevented by Mesna • Treatment is steroids • travel in cycle () → acral rashes () → acrolein |
↳ Ifosfamide (Nitrogen mustards) | S/E • Hemorrhagic cystitis If Cycle → irunn irunn hemorrhagic cystitis avum |
↳ Busulfan | S/E • Pulmonary fibrosis |
↳ Nitrosoureas ⤿Carmustine (BCNU) ⤿Lomustine (CCNU) ⤿Semustine (Methyl CCNU) | S/E • Delayed neutropenia Nitrosurea → Neutropenia |
↳ Procarbazine | S/E • disulfiram-like reaction Caril povumbo → no alcohol Pro car → poka adikkilla → NO PULM Fibrosis (Carmust → sada car → Pulmfibrosis) |
↳ Mitomycin C | • Used in Ca UB • Used topically for ◦ Subglottic stenosis ◦ Superficial bladder cancer |
↳ Temozolamide | • Cause DNA guanine methylation • DOC gliomas • Temu (temozolomide) nnu vangiya globe (glioma) |
↳ Anthracycline ⤿ Doxorubicin ⤿ Donorubicin ⤿ Epirubicin | S/E • All Cause Cardiotoxicity ↳ Reduced by giving Dexrazoxane (Iron scavenger) • Red urine • Radiation recall dermatitis • Radiation from red ruby from anthra caused cardiotoxic |
↳ Melphalan | • Used for multiple myeloma • Mel → Mul myl |
↳ Dactinomycin | ㅤ |
OTHERS | ㅤ |
↳ Hydroxyurea | MOA: ⛔ Ribonucleotide Reductase Uses • Polycythemia Vera • Essential Thrombocythemia • Sickle Cell Disease |
Bortezomib + Lenalidomide + Dexamethasone | Use: Multiple Myeloma |
NEW DRUGS
Drug | Target / Mechanism | Use / Indication |
Vismodegib | Sonic Hedgehog pathway inhibitor | Basal cell carcinoma |
Osimertinib | EGFR T790M mutation inhibitor | Adenocarcinoma lung |
Belimumab | BLyS inhibitor | SLE |
Teprotumumab | IGF-1 receptor inhibitor | Thyroid eye disease |
Elacestrant, Fulvestrant | SERD – estrogen receptor degrader | Breast cancer |
Teplizumab | Anti-CD3 antibody | Type 1 DM |
Omaveloxolone | Nrf2 activator | Friedreich’s ataxia |
Ravulizumab, Rozanolixizumab | Complement inhibition / FcRn inhibition | Myasthenia gravis |
Daprodustat | Hypoxia-inducible factor stabilizer | Anemia of CKD |
Vonoprazan | Reversible PPI (K⁺-competitive acid blocker) | Acid-peptic disease |
Palivizumab | Anti-RSV F protein | RSV prophylaxis in high-risk infants |
Cetuximab, Panitumumab | EGFR inhibitor | Adenocarcinoma lung, Colon cancer |
Emicizumab | Factor VIII mimetic | Hemophilia A |
Natalizumab | α4-integrin inhibitor | MS |
ㅤ | S/E: PML | ㅤ |
IFN-α | From leukocytes | Hepatitis B, Hepatitis C |
IFN-β | From fibroblasts | MS |
IFN-γ | From T-cells | Chronic granulomatous disease |
Aldesleukin | IL-2 (Immunotherapy) | RCC, Melanoma |
Biologic Drugs (Autoimmune / Inflammatory)
Drug | Target | Use |
Ixekizumab, Secukinumab | IL-17 inhibitor | Psoriasis, RA |
Risankizumab, Guselkumab, Tildrakizumab | IL-23 inhibitor | Psoriasis, RA |
Ustekinumab | IL-12, IL-23 inhibitor | Psoriasis, RA |
Anticancer Small-Molecule Inhibitors
Drug | Target | Indication |
Alectinib, Crizotinib | ALK | Non-small cell lung cancer |
Erlotinib, Gefitinib, Afatinib | EGFR (L858R mutation) | NSCLC |
Imatinib, Dasatinib, Nilotinib | BCR-ABL | CML, ALL, GISTs |
Ruxolitinib | JAK1/2 | Polycythemia vera |
Bortezomib, Ixazomib, Carfilzomib | Proteasome inhibitor | Multiple myeloma, Mantle cell lymphoma |
ㅤ | Mechanism | G2-M arrest → apoptosis |
ㅤ | S/E | ↑ HSV reactivation |
Vemurafenib, Encorafenib, Dabrafenib | BRAF | Melanoma |
ㅤ | ㅤ | Hairy cell leukemia, Papillary thyroid cancer, Colon cancer |
Palbociclib | CDK 4/6 inhibitor | Breast cancer |
ㅤ | Mechanism | G1-S arrest → apoptosis |
Olaparib | PARP inhibitor (↓ DNA repair) | Breast, ovarian, Pancreatic, prostate cancers |
ㅤ | Association | BRCA1 / BRCA2 |
Alemtuzumab | CD52 | CLL |
Drugs Causing Pulmonary Fibrosis
Mnemonic:
- CYCLOphosphomide,
- CARmustine,
- BUSulphan,
- MethoTRUCKsate,
- AmioDaRONE,
- BLEOmycin
Antimetabolites
- These are S Phase Specific
Folic acid function
- In Methotrexate
- Supplementation
- In Purine and Pyrimidine drugs
- Potentiate action
Drugs Affecting Purine Metabolism
- Cladribine:
- DOC for Hairy cell Leukamia
- Mnemonic: Clara → hairy
- Fludarabine:
- DOC for CLL
- Mnemonic: Flood → Call
ADA Inhibition
- Cladribine, Pentostatin
- ⛔ ADA
- NOTE: SCID
- ADA deficiency
- Lesch Neyhan syndrome
- ⛔ HGPRT
Drugs Affecting Pyrimidine Metabolism
In Ca Colon
- FOLFOX
- Folinic Acid + 5FU + Oxaliplatin
- FOLFIRI
- Folinic Acid + 5FU + Irinotecan
Side effects
- Common Adverse Effects
- BM Suppression
- Alopecia
- Mucositis → Diarrhea
- Hyperuricemia
- Nausea and vomiting (CINV)
- Cytarabine
- Cerebellar toxicity
- Anthracyclines & Actinomycin D, Gemcitabine
- Radiation recall dermatitis
- erythematous rashes in areas previously radiation exposed areas
Rx for N & V
Type | Drug of Choice |
Early CINV < 24 hours | 5HT3 Antagonists - Ondansetron - Granisetron - Palonosetron |
Delayed CINV > 24 hours | NK1 / Substance P Antagonists - Aprepitant - Rolapitant |
ㅤ | • Dexamethsone |
Nail pigmentation causing drugs
- Phenothiazines
- Chlorpromazine
- Used for DM and DI
- S/E: SIADH, Disulfiram like reaction
- Chloroquine
- Minocycline
- Queen meena for magazine → put nail lacquer
Minocycline:
- Given for acne
- Leads to blue-black pigmentation on acne scars
- Black thyroid
- Due to deposition of iron chelates with minocycline
- Also leads to lupus-like reaction
- Mnemonic: Meena de mugath blue black vann
TARGETED ANTICANCER DRUGS
SMALL MOLECULES | ㅤ |
Tyrosine Kinase Inhibitors | • Orally effective • All end with ‘nib’ |
↳ Imatinib | • CML, GIST For CML ◦ I-N-D ◦ I - Imatinib [DOC] ◦ N - Nilotinib ◦ D - Dasatinib For GIST ◦ Get (GIST) Suni (Sunitinib) Immediately () ◦ Sunitinib ◦ Imatinib [DOC] ◦ Regorafenib |
↳ Lapatinib | • Breast Ca |
↳ Sorafenib | • HCC |
MONOCLONAL ANTIBODIES | • End with ‘MAB’ • Injectable |
AGAINST CD20 | ㅤ |
↳ Rituximab | • Non-Hodgkin Lymphoma • CLL • Mono → think of a single girl → fresh to college • 20 (CD20) year old Ritu (rituxi) → Nahi Hoti Late (NHL) for College (CLL) • She Jaffarum (EGFR ANTAGONISTS) ayi Set (Cetuximab) ayi → Pani (Panitumumab) kitti → backil (Colorectal cancer) • Trust (tratsuzumab) cheythapo breast peruthu (Pertuzuman) → Heart poi (cardotoxic) |
AGAINST HER – 2 | • Use: breast cancer |
↳ Trastuzumab | • S/E: Cardiotoxic |
↳ Pertuzumab | • Trust (tratsuzumab) cheythapo breast peruthu (Pertuzuman) → Heart poi (cardotoxic) |
EGFR ANTAGONISTS: | • Use: Colorectal carcinoma |
↳ Cetuximab | ㅤ |
↳ Panitumumab | ㅤ |
Immune Checkpoint Mechanism and Inhibitors
Checkpoint | Acts where | Example inhibitor |
CTLA-4 | Lymph nodes (early) | Ipilimumab [first FDA-approved - (melanoma)] LN → Ikkilakkum |
PD - 1 R | Peripheral tissues (late) | Nivolumab, Pembrolizumab Tea → Ni (Nivolu) Pemranothi () |
PD - L1 | Tumor/APCs | Atezolizumab, Durvalumab, Avelumab Durvasavu (Durvalumab) tumor () Avil () aakki thinnu (Ate) |
Cancer | Approved ICIs |
Melanoma | Ipilimumab (CTLA-4), Nivolumab (PD-1), Pembrolizumab (PD-1) |
NSCLC | Pembrolizumab (PD-1), Nivolumab (PD-1), Atezolizumab (PD-L1), Durvalumab (PD-L1) |
Renal Cell Carcinoma | Nivolumab (PD-1), Ipilimumab (CTLA-4) |
Hepatocellular Carcinoma | Atezolizumab (PD-L1) + Bevacizumab (anti-VEGF) |
Hodgkin Lymphoma | Nivolumab (PD-1), Pembrolizumab (PD-1) |
- Normal Function:
- PD-1: Receptor on T-cells.
- PDL-1: Ligand on normal cells.
- Interaction inhibits T-cells → Prevents attack on normal cells.
- This is called the immune checkpoint.
- Immune Checkpoint Inhibitors:
- Monoclonal antibodies against PD-1 or PDL-1.
- Block interaction → Reactivate T-cells.
- T-cells kill tumor cells.
- Adverse Effect:
- May cause autoimmune diseases.
- Example: Autoimmune hepatitis.
- Drugs
- Mnemonic: “L → umab”
- Mnemonic: New Drugs Act At Immune Check Point
Non Small Cell Lung Ca
- If Mutation absent
- Chemotherapy (Cisplatin + Etoposide) +
- ICP Inhibitors (Pembrolizumab/Atezolizumab)
OR - Double ICP Inhibitors
- Nivolumab + Ipilimumab
Clinical Trials | Condition | Rx |
KEYNOTE-158 trial: | • MSI-H/dMMR endometrial cancer | Pembrolizumab |
KEYNOTE-146 trial: | • Advanced endometrial cancer | Pembrolizumab |
Keynote 189 Trial | • Non Small cell Lung Ca | Chemotherapy + Pembrolizumab |
IMMUNOSUPPRESSANTS
1. STEROIDS | ㅤ |
2. TARGETING CALCINEURIN PATHWAY | ㅤ |
Inhibit formation of IL-2 | • IL2 formation → Pooping • inhibited by tucking () with a cycle () |
↳ Cyclosporine | ㅤ |
↳ Tacrolimus | • 50–100× more potent |
Inhibit IL 2 Receptor (CD25) | • IL 2 R → toilet → duck and basil in toilet |
↳ Daclizumab | ㅤ |
↳ Basiliximab | ㅤ |
Inhibit action of IL - 2 | • Last → Sir () Everestil () tuuri (TOR) • ⛔ mTOR |
↳ Sirolimus | ㅤ |
↳ Everolimus | ㅤ |
3. BIOLOGICAL AGENTS | • Formed by recombinant DNA technology • TNF-α inhibitors • ACE INhibitor GOLI |
↳ Adalimumab | A |
↳ Certolizumab | C |
↳ Etanercept | E |
↳ INfliximab | INhibitor |
↳ GOLImumab | GOLI |
- α (TNF α) EEttane (Etanacerpt) → Pain Inflict (Infliximab) cheyyan → Goli (Golimumab) vach scrotathil (certolizumab) Adikkanam (Adalimumab)
Breast Cancer chemotherapy drugs:
ㅤ | 1st line | No response |
ER Positive | ER il | ㅤ |
Premenopausal | • Tamoxifen Premen girl - we Tame | ㅤ |
Postmenopausal | • Letrozole Postmen girl - she Let in, but Full Elastic | • Fulvestrant • Elacestrant (ESR-1 mutation) |
Her2 Positive | ㅤ | ㅤ |
ㅤ | • Trastuzumab (DOC) Her hole - Tight & Lap Peruthu Neeradichu | • Neratinib • Pertuzumab • Lapatinib |
Triple Negative | ㅤ | ㅤ |
ㅤ | DCP • Doxorubicin • Carboplatin • Paclitaxel Threesome → Do () in Car () 4 Paisa () at Olaparambu () with Wife (Pembroli) | Add on • Pembrolizumab BRCA mutation • Olaparib |
The Nobel Prize in Physiology or Medicine, 2018 was awarded to James P. Allison and Tasuku Honjo for which of the following discoveries?
A. Discovery of mechanisms of autophagy
B. Discoveries of molecular mechanisms controlling the circadian rhythm
C. Discovery of cancer therapy by inhibition of negative immune regulation
D. The discovery that matures cells can be reprogrammed to become pluripotent
B. Discoveries of molecular mechanisms controlling the circadian rhythm
C. Discovery of cancer therapy by inhibition of negative immune regulation
D. The discovery that matures cells can be reprogrammed to become pluripotent
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