Anti-Cancer Drugs😍

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
Bleomycin: 
• Flagellated pigmentation of skin
Bleomycin:
Flagellated pigmentation of skin
  • Christians () blew () with chlorine () and asparagus ()
Anticancer drugs can be divided into
  1. Cytotoxic
  1. Targeted

Classification

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G₂ phase
Bleomycin
• Causes DNA strand breaks
Marrow sparing

S/E
Pulmonary fibrosis
Flagellated pigmentation of skin
Blew horns on skin → pigmentation
S Phase
Affect Folic Acid Metabolism
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
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
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
Gemcitabine
DOC for Pancreatic carcinoma
Pancreas is a gem
M Phase
Win (vincristine, vinblastine) a Packet (Paclitaxel)
by rotating spindle
Microtubule Inhibitors
Taxanes
Hyperstabilization of microtubules
Tax stabilise society
Paclitaxel
Vinca alkaloids
• Disruption of microtubules

S/E
Peripheral neuropathy
SIADH
Vincristine
Marrow sparing
Vinblastine
Topoisomerase Inhibitors
Top (Topoisomerase) → Irene (Irenetecan) nte top sidilott (Etoposide) poi → ruby (Donorubi……) kandu
Topo II
Etoposide
Teniposide
Topo I
Irinotecan
Used for colorectal carcinoma
Cholinergic S/E
Topotecan
Cell Cycle–Independent Drugs
Platinum Compounds
Cisplatin
S/E
Ototoxicity
Nephrotoxicity (⛔ Reabsorption in distal tubules)
Hypokalemia
Hypomagnesemia
Hypocalcemia
Hypophosphatemia
Max Nausea & Vomiting

Prevention
1-2 L NSChloride diuresisinactivate 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)

If (Ifs) Bus (Busu) Not (Nitro) Present (Procar) Take (Temo) My (Melph, Mito) Cycle (Cyc)
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
• 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
OTHERS
Hydroxyurea
MOA: ⛔ Ribonucleotide Reductase

Uses
Polycythemia Vera
Essential Thrombocythemia
Sickle Cell Disease
Bortezomib + Lenalidomide + Dexamethasone
Use: Multiple Myeloma
Antifibrotic agent
Pirfenidone
Used in Idiopathic pulmonary fibrosis (IPF)
IPF vannal tell pt → drink feni → ur done (fenidone)

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
S/E: PML
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
Mechanism
G2-M arrest → apoptosis
S/E
↑ HSV reactivation
Vemurafenib,
Encorafenib,
Dabrafenib
BRAF
Melanoma
Hairy cell leukemia,
Papillary thyroid cancer,
Colon cancer
Palbociclib
CDK 4/6 inhibitor
Breast cancer
Mechanism
G1-S arrest → apoptosis
Olaparib
PARP inhibitor (↓ DNA repair)
Breast, ovarian,
Pancreatic, prostate cancers
Association
BRCA1 / BRCA2
Alemtuzumab
CD52
CLL

Cytotoxic Drugs

Common Adverse Effects

  • BM Suppression
  • Alopecia
  • Mucositis → Diarrhea
  • Hyperuricemia
  • Nausea and vomiting (CINV)

1. Alkylating Agents

  • Mnemonic: Must (mustine drugs) buy Mighty (mitomycin c,melphalan) Car (Procarbazine) Bus (Busulfan) Cycle (cyclophosp) from Temu () → ↓↓ Price →→ ↓↓ H+ (Temu → alkylating agent)

Drugs:

  • If – Ifosfamide
  • Bus – Busulfan
  • Not – Nitrosoureas
    • Carmustine (BCNU)
    • Lomustine (CCNU)
    • Semustine (Methyl CCNU)
  • Present – Procarbazine
  • Take – Temozolomide
  • My – Melphalan, Mitomycin C
  • Cycle – Cyclophosphamide

Important Points Regarding Alkylating Agents

Drug
Use & S/E
Mnemonic
Cyclophosphamide:
Cause Hemorrhagic cystitis
Cause SIADH
Cause Pulmonary fibrosis
Cycle and Bus → Poka adikkum → Pulm fibrosis
Ifosfamide:
Cause Hemorrhagic cystitis
If Cycle → irunn irunn hemorrhagic cystitis avum
Busulfan:
Cause pulmonary fibrosis
Nitrosoureas:
Cause Delayed neutropenia
Nitrosurea → Neutropenia
Procarbazine:
Cause disulfiram-like reaction
Caril povumbo → no alcohol

Pro car → poka adikkilla → NO PULM Fibrosis

(
Carmust → sada car → Pulmfibrosis)
Temozolomide:
DOC for gliomas
Temu (temozolomide) nnu vangiya globe (glioma)
Melphalan:
Used for multiple myeloma
Mel → Mul myl
Mitomycin-C:
Used topically for
Subglottic stenosis
Superficial bladder cancer

Hemorrhagic cystitis

  • Caused by cyclophosphamide and ifosmide
  • Metabolite responsible is acrolein
    • travel in cycle → acral rashes → acrolein
  • Prevented by Mesna
  • Treatment is steroids

Drugs Causing Pulmonary Fibrosis

Mnemonic: 

  • CYCLOphosphomide,
    • notion image
  • CARmustine,
    • notion image
  • BUSulphan,
    • notion image
  • MethoTRUCKsate,
    • notion image
  • AmioDaRONE,
    • notion image
  • BLEOmycin
    • notion image

Antifibrotic agent

  • Pirfenidone
  • Used in Idiopathic pulmonary fibrosis (IPF)
  • IPF vannal tell pt → drink feni → ur done (fenidone)

2. Antimetabolites

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  • These are S Phase Specific
  • Folic acid function
    • In Methotrexate
      • Supplementation
    • In Purine and Pyrimidine drugs
      • Potentiate action

a. Drugs affecting Folic Acid Metabolism

  • Example: Methotrexate
  • Act by inhibiting dihydrofolate reductase enzyme
  • of Methotrexate:
    • 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

b. Drugs Affecting Purine Metabolism

  • 6 - Mercaptopurine: Hepatotoxic
  • 6 - Thioguanine: Hepatotoxic
  • Cladribine: 
    • DOC for Hairy cell Leukamia
    • Mnemonic: Clara → hairy
  • Fludarabine:
    • DOC for CLL
    • Mnemonic: Flood → Call
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  • Cladribine, Pentostatin
    • ⛔ ADA
    • NOTE: SCID
      • ADA deficiency
  • Lesch Neyhan syndrome
    • ⛔ HGPRT

c. Drugs Affecting Pyrimidine Metabolism

egyptian mummy (pyramid) wearing a cape (capecitabin) sitting (citarabin) with a big gem (gemcitabin) → 5 fluorescent (5 FU) green lamp
egyptian mummy (pyramid) wearing a cape (capecitabin) sitting (citarabin) with a big gem (gemcitabin) → 5 fluorescent (5 FU) green lamp
 
  • Capecitabine
    • Prodrug
    • Hand and foot syndrome
      • Capecitabine > 5-Fluorouracil [5-FU]
  • 5-Fluorouracil [5-FU]
  • Gemcitabine
    • DOC for Pancreatic carcinoma
    • Pancreas is a gem
  • Cytarabine
    • Cause cerebellar side effects
    • Sit when ataxia (cerebellar s/e)

In Ca Colon

  • FOLFOX
    • Folinic Acid + 5FU + Oxaliplatin
  • FOLFIRI
    • Folinic Acid + 5FU + Irinotecan

3. Drugs Acting on Mitotic Spindle

  • Specific for M-Phase of cell cycle
      1. Formation ⛔
          • Vincristine
            • Marrow sparing anticancer drug
          • Vinblastine

          S/E for both

          • Peripheral neuropathy
          • SIADH
      1. Breakdown ⛔
          • Paclitaxel
  • Mnemonic:
    • Win (vincristine, vinblastine) a Packet (Paclitaxel) → by rotating spindle

4. Topoisomerase Inhibitors

  • Topoisomerase I inhibitors
    • Irinotecan
      • Used for colorectal carcinoma
      • Cholinergic Side effects
  • Topoisomerase II inhibitors
    • Etoposide
    • Anthracyclines
      • 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
  • Mnemonic: Top (Topoisomerase) → Irene (Irenetecan) nte top sidilott (Etoposide) poi → ruby (Donorubi……) kandu

Side effects

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  • Cytarabine
    • Cerebellar toxicity
  • Anthracyclines & Actinomycin D, Gemcitabine
    • Radiation recall dermatitis
      • erythematous rashes in areas previously radiation exposed areas

Cisplatin

  • S/E Triad
      1. Ototoxicity
      1. Nephrotoxicity
          • It particularly affects the reabsorption in the distal tubules, causing:
            • Hypomagnesemia
            • Hypokalemia
            • Hypocalcemia
            • Hypophosphatemia
          • Prevention
            • 1-2 L NSChloride diuresisinactivate cisplatin
            • then Mannitol → to throw Cisplatin from body
            • then Amifostine → to reduce side effects of radiotherapy
          • Mnemonic: Sis nu Plate kodukk → Amikk first (Amfostine) kodukk
      1. Max Nausea & Vomiting
          • 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
              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:

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  • 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
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TARGETED ANTICANCER DRUGS

A. SMALL MOLECULES

SMALL MOLECULES
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
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
Panitumumab
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Immune Checkpoint Mechanism and Inhibitors

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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)
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  • Normal Function:
    • PD-1: Receptor on T-cells.
    • PDL-1: Ligand on normal cells.
    • Interaction inhibits T-cellsPrevents 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

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  • 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

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1. STEROIDS
2. TARGETING CALCINEURIN PATHWAY
Inhibit formation of IL-2
IL2 formation → Pooping
inhibited by tucking () with a cycle ()
Cyclosporine
Tacrolimus
50–100× more potent
Inhibit IL 2 Receptor (CD25)
IL 2 R → toilet → duck and basil in toilet
Daclizumab
Basiliximab
Inhibit action of IL - 2
Last → Sir () Everestil () tuuri (TOR)
⛔ mTOR
Sirolimus
Everolimus
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)
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Breast Cancer chemotherapy drugs:

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1st line
No response
ER Positive
ER il
Premenopausal
Tamoxifen

Premen girl
- we Tame
Postmenopausal
Letrozole

Postmen girl
- she Let in, but Full Elastic
Fulvestrant
Elacestrant (ESR-1 mutation)
Her2 Positive
• Trastuzumab (DOC)

Her hole - Tight & Lap Peruthu Neeradichu
Neratinib
Pertuzumab
Lapatinib
Triple Negative
DCP
Doxorubicin
Carboplatin
Paclitaxel

Threesome → Do () in Car () 4 Paisa () at Olaparambu () with Wife (Pembroli)
Add on
Pembrolizumab

BRCA mutation
Olaparib

Others

  • Hydroxyurea
    • Polycythemia Vera
    • Essential Thrombocythemia
    • Sickle Cell Disease
    • MOA: ⛔ Ribonucleotide Reductase
  • Multiple Myeloma:
    • Bortezomib + Lenalidomide + Dexamethasone
 
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
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