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HH M2 CA1 GENPATH > GENPATH Anti Cancer Drugs > Flashcards

GENPATH Anti Cancer Drugs Flashcards

1
Q

5-Fluorouracil’s main MOA is the inhibition of […]

A

5-Fluorouracil’s main MOA is the inhibition of Thymidylate Synthase (TS)

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2
Q

Alkylating agent for anti-cancer

mechanism of action:
[…]

examples:
[…]

A

Alkylating agent for anti-cancer

mechanism of action:
reactive alkyl group forms covalent bonds with DNA –> DNA crosslinkage OR strand breakage –> prevent further DNA replication and transcription

examples:
- Cyclophosphamide
- Chloromabucil
- Dacarbazine

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3
Q

Anti-metabolites chemotherapy drug

mechanism:
[…]

example:
- […]
- […]
- 6-thioguanine
- 6-mercaptopurine
- cytosine arabinoside
- gemcitabine

A

Anti-metabolites chemotherapy drug

mechanism:
inhibit nucleic acid (purine & pyrimidine) synthesis for DNA replication

example:
- methotrexate
- 5-fluorouracil
- 6-thioguanine
- 6-mercaptopurine
- cytosine arabinoside
- gemcitabine

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4
Q

Cyclophosphamide is what class???

[…]

A

Cyclophosphamide is what class???

Alkylating yo

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5
Q

Cytotoxic antibiotics

Mechanisms:
[…]

Examples:
Anthracyclines:
[…]
- Daunorubicin
- idarubicin
- epirubicin
Others:
- mitomycin C
- Bleomycin

Unique side effect:
[…] (IMPT!)

A

Cytotoxic antibiotics

Mechanisms:

**1. interfere with DNA replication
2. generates ROS which damages DNA and cell membranes
3. inhibition of topoisomerase II
4. alter membrane fluidity and ion transport

Examples:
Anthracyclines:
- Doxorubicin (most impt)
- Daunorubicin
- idarubicin
- epirubicin
Others:
- mitomycin C
- Bleomycin

Unique side effect:
Cardiac toxicity (IMPT!)

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6
Q

Methotrexate inhibits […] enzyme, hence inhibiting […] synthesis

A

Methotrexate inhibits Dihydrofolate Reductase (DHFR) enzyme, hence inhibiting tetrahydrofolate synthesis

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7
Q

Microtubule inhibitors:

Mechanisms
[…]

Examples
[…]

Unique adverse effects:
[…]

A

Microtubule inhibitors:

Mechanisms
bind to beta subunit of tubilin –> prevent elongation/shortening of microtubule –> prevent cell division

Examples
**Vinca alkaloids (from Periwinkle):
- Vinblastine
- Vincristine
- Vinorelbine
Taxanes (From Yew trees):
- Paclitaxel
- Docetaxel
- Carbazitaxel

Unique adverse effects:
- Peripheral neuropathy
- Bradycardia (esp taxol)

Similar to anti-metabolites, microtubule inhibitors are cell cycle specific

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8
Q

Name 2 TKIs that binds to kinase domain of ErbB

[…]

A

Name 2 TKIs that binds to kinase domain of ErbB

Gefi-tinib & Lapa-tinib

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9
Q

Platinum analogues for anticancer

mechanism:
[…]

example:
[…]

unique adverse effects:
[…]

A

Platinum analogues for anticancer

mechanism:
Adduction to DNA strands –> causes intra-strand crosslink/DNA-protein crosslink –> prevention of cell replication

example:
**- cisplatin
- carboplatin
- oxaliplatin

**unique adverse effects:
- nephrotoxicity
- peripheral sensory neuropathy

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10
Q

Then cisplatin is what class??

[…]

A

Then cisplatin is what class??

Platinum analogues bro

All the platinum analogues end with platin. ez dab ez life 幸福就是这么简单

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11
Q

Topoisomerase inhibitors

Mechanism
[…]

Example:
Type 1 inhibitors
[…]
Type 2 inhibitors
- Amsacrine
[…]

A

Topoisomerase inhibitors

Mechanism
Inhibit type 1/2 topoisomerase –> disruption of appropriate DNA supercoiling, interfering with transcription and replication of DNA

Example:
Type 1 inhibitors
-* Irinotecan *
-* Topotecan*
Type 2 inhibitors
- Amsacrine
-* Etoposide*
-* teniposide*

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12
Q

Type of cell death by chemotherapy: […]

A

Type of cell death by chemotherapy: apoptosis

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13
Q

What are the 2 approaches of T-cell immunotherapy?

[…]

A

What are the 2 approaches of T-cell immunotherapy?

  • **CAR T-cell **(T cells engineered to express CARs that recognise tumour cells)
  • Immune checkpoint inhibitors (block CTLA-4/PD-L1/2)
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14
Q

What are the 3 main categories of anticancer drugs?

  1. […]
  2. […]
  3. […]
A

What are the 3 main categories of anticancer drugs?

  1. Cytotoxic drugs (PACMAT)
  2. Endocrine agents
  3. Targeted therapies
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15
Q

What are the 3 main mechanism of action of therapeutic antibodies?

A

What are the 3 main mechanism of action of therapeutic antibodies?

**- Neutralizing Abs (to VEGF)
- Effector-mediated cytotoxicity (ADCC/CDC)
- Ab Drug Conjugates (drug hitchhike endocytosed ab)

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16
Q

What are the 3 main types of targeted therapeutic drugs for cancer?

[…]

A

What are the 3 main types of targeted therapeutic drugs for cancer?

  • Tyrosine kinase inhibitors (TKI)
  • Proteosome inhibitors
  • Monoclonal antibodies (mAbs)
17
Q

What are the 6 classes anticancer cytotoxic drugs?** (IMPT)**

  • […]
  • […]
  • […]
  • […]
  • […]
  • […]
A

What are the 6 classes anticancer cytotoxic drugs? (IMPT)

  • Platinating drugs
  • Alkylating agents
  • Cytotoxic Antibiotics
  • Microtubule inhibitors
  • Anti-metabolites
  • Topoisomerase inhibitors
18
Q

What are the advantages of combination chemotherapy?

  • […]
  • […]
  • […]
A

What are the advantages of combination chemotherapy?

  • Maximal cell killing
  • Drug synergy
  • Prevent/slow development of drug resistance
19
Q

What are the common chemotherapy side effects?

Common acute toxicity
- […]
- […]
- […]
- […]

Late organ toxicity
- […]
- […]
- […]
- […]
- […]
- […]
- […]
- […]
- […]

A

What are the common chemotherapy side effects?

Common acute toxicity
- myelosuppression
- Nausea, vomitting, GI effects
- Mucous membrane ulceration
-* Alopecia*

Late organ toxicity
- cardiotoxicity
- Pulmonary toxicity
- Nephrotoxicity
- Neurotoxicity
- Haematologic and immunologic impairment (Anaemia, fatigue, immunodeficiency, thrombocytopenia, etc) **
- Secondary malignancies
-* Teratogenicity*
-* Endocrine disruption*
-* Premature menopause, infertility***

20
Q

What are the highly proliferative tissues in the body (other than tumors themselves) that are affected by chemotherapic drugs?

eg:
[…]

A

What are the highly proliferative tissues in the body (other than tumors themselves) that are affected by chemotherapic drugs?

eg:
**1. skin
2. hair follicle
3. bone marrow
4. mucous membrane

21
Q

What are the treatment options for cancer?

  1. […]
  2. […]
  3. […]
  4. Cryotherapy (liquid N2)/ Thermotherapy (microwave or radiofrequency)
  5. molecular targeted therapy (mAbs, small inhibitors)
    6.** Biological response modifiers** (immuno-oncology)
  6. **Combination and multimodality therapies **
A

What are the treatment options for cancer?

  1. Surgery (resection or transplantation)
  2. Radiotherapy
  3. Pharmacotherapy/Chemotherapy
  4. **Cryotherapy **(liquid N2)/ **Thermotherapy **(microwave or radiofrequency)
  5. molecular targeted therapy (mAbs, small inhibitors)
  6. Biological response modifiers (immuno-oncology)
  7. Combination and multimodality therapies
22
Q

What are the various roles of cancer pharmacotherapy?

  1. Induction: aim at achieving significant reduction in tumour burden
  2. Curative: For […] cancers
    3.** Neo-adjuvant**: […]-operative therapy to downstage tumour burden before surgery/radiotherapy
  3. Adjuvant: […]-operative therapy
  4. Maintenance: prolonged low dose therapy
  5. Palliative/Salvage: treatment for […] disease
  6. Combination with radiotherapy as radiation sensitiser: treatment of head and neck cancer, cervical cancer
A

What are the various roles of cancer pharmacotherapy?

  1. Induction: aim at achieving significant reduction in tumour burden
  2. Curative: For metastatic cancers
  3. Neo-adjuvant: pre-operative therapy to downstage tumour burden before surgery/radiotherapy
  4. Adjuvant:* post*-operative therapy
  5. Maintenance: prolonged low dose therapy
  6. Palliative/Salvage: treatment for metastatic/advanced disease
  7. Combination with radiotherapy as radiation sensitiser: treatment of head and neck cancer, cervical cancer
23
Q

Why are chemotherapeutic drugs given in cycles?

[…]
- […]
- […]
- […]

A

Why are chemotherapeutic drugs given in cycles?

l**og kill hypothesis!! A fixed percentage of tumor cells are killed per cycle
- One-log drug kills 90% of the tumour cells
- two-log drug kills 99%
- three log kills 99.9%

HH M2 CA1 GENPATH (9 decks)

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