GENPATH Anti Cancer Drugs Flashcards
5-Fluorouracil’s main MOA is the inhibition of […]
5-Fluorouracil’s main MOA is the inhibition of Thymidylate Synthase (TS)
Alkylating agent for anti-cancer
mechanism of action:
[…]
examples:
[…]
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
Anti-metabolites chemotherapy drug
mechanism:
[…]
example:
- […]
- […]
- 6-thioguanine
- 6-mercaptopurine
- cytosine arabinoside
- gemcitabine
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
Cyclophosphamide is what class???
[…]
Cyclophosphamide is what class???
Alkylating yo
Cytotoxic antibiotics
Mechanisms:
[…]
Examples:
Anthracyclines:
[…]
- Daunorubicin
- idarubicin
- epirubicin
Others:
- mitomycin C
- Bleomycin
Unique side effect:
[…] (IMPT!)
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!)
Methotrexate inhibits […] enzyme, hence inhibiting […] synthesis
Methotrexate inhibits Dihydrofolate Reductase (DHFR) enzyme, hence inhibiting tetrahydrofolate synthesis
Microtubule inhibitors:
Mechanisms
[…]
Examples
[…]
Unique adverse effects:
[…]
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
Name 2 TKIs that binds to kinase domain of ErbB
[…]
Name 2 TKIs that binds to kinase domain of ErbB
Gefi-tinib & Lapa-tinib
Platinum analogues for anticancer
mechanism:
[…]
example:
[…]
unique adverse effects:
[…]
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
Then cisplatin is what class??
[…]
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
Topoisomerase inhibitors
Mechanism
[…]
Example:
Type 1 inhibitors
[…]
Type 2 inhibitors
- Amsacrine
[…]
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*
Type of cell death by chemotherapy: […]
Type of cell death by chemotherapy: apoptosis
What are the 2 approaches of T-cell immunotherapy?
[…]
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)
What are the 3 main categories of anticancer drugs?
- […]
- […]
- […]
What are the 3 main categories of anticancer drugs?
- Cytotoxic drugs (PACMAT)
- Endocrine agents
- Targeted therapies
What are the 3 main mechanism of action of therapeutic antibodies?
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)
What are the 3 main types of targeted therapeutic drugs for cancer?
[…]
What are the 3 main types of targeted therapeutic drugs for cancer?
- Tyrosine kinase inhibitors (TKI)
- Proteosome inhibitors
- Monoclonal antibodies (mAbs)
What are the 6 classes anticancer cytotoxic drugs?** (IMPT)**
- […]
- […]
- […]
- […]
- […]
- […]
What are the 6 classes anticancer cytotoxic drugs? (IMPT)
- Platinating drugs
- Alkylating agents
- Cytotoxic Antibiotics
- Microtubule inhibitors
- Anti-metabolites
- Topoisomerase inhibitors
What are the advantages of combination chemotherapy?
- […]
- […]
- […]
What are the advantages of combination chemotherapy?
- Maximal cell killing
- Drug synergy
- Prevent/slow development of drug resistance
What are the common chemotherapy side effects?
Common acute toxicity
- […]
- […]
- […]
- […]
Late organ toxicity
- […]
- […]
- […]
- […]
- […]
- […]
- […]
- […]
- […]
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***
What are the highly proliferative tissues in the body (other than tumors themselves) that are affected by chemotherapic drugs?
eg:
[…]
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
What are the treatment options for cancer?
- […]
- […]
- […]
- Cryotherapy (liquid N2)/ Thermotherapy (microwave or radiofrequency)
-
molecular targeted therapy (mAbs, small inhibitors)
6.** Biological response modifiers** (immuno-oncology) - **Combination and multimodality therapies **
What are the treatment options for cancer?
- Surgery (resection or transplantation)
- Radiotherapy
- Pharmacotherapy/Chemotherapy
- **Cryotherapy **(liquid N2)/ **Thermotherapy **(microwave or radiofrequency)
- molecular targeted therapy (mAbs, small inhibitors)
- Biological response modifiers (immuno-oncology)
- Combination and multimodality therapies
What are the various roles of cancer pharmacotherapy?
- Induction: aim at achieving significant reduction in tumour burden
-
Curative: For […] cancers
3.** Neo-adjuvant**: […]-operative therapy to downstage tumour burden before surgery/radiotherapy - Adjuvant: […]-operative therapy
- Maintenance: prolonged low dose therapy
- Palliative/Salvage: treatment for […] disease
- Combination with radiotherapy as radiation sensitiser: treatment of head and neck cancer, cervical cancer
What are the various roles of cancer pharmacotherapy?
- Induction: aim at achieving significant reduction in tumour burden
- Curative: For metastatic cancers
- Neo-adjuvant: pre-operative therapy to downstage tumour burden before surgery/radiotherapy
- Adjuvant:* post*-operative therapy
- Maintenance: prolonged low dose therapy
- Palliative/Salvage: treatment for metastatic/advanced disease
- Combination with radiotherapy as radiation sensitiser: treatment of head and neck cancer, cervical cancer
Why are chemotherapeutic drugs given in cycles?
[…]
- […]
- […]
- […]
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%
