Medical Pharmacology Practice Questions: Chapter 33-34 Inhibitor of RAF Kinase Dabrafenib (Tafinlar)

Medical Pharmacology Practice Questions: Inhibitor of RAF Kinase Dabrafenib (Tafinlar)

Dabrafenib (Tafinlar):
1. Oral, bioavailable.
2. Inhibitor of mutated BRAF kinases
3. Both
4. Either
Dabrafenib inhibits tumor cell growth which is depended on the constitutively activated mutated BRAF.
1. True
2. Alz
Clinical use(s):
1. Approved for treatment of patients with metastatic melanoma, in combination with trametinib.
2. Approved for patients with non-small cell lung cancer (NSCLC) with BRAF mutations (given in combination with trametinib)
3. Both
4. Neither
Dabrafenib (as well as vemurafenib):
1. Only dabrafenib exhibits greater clinical benefits compared to dacarbazine (cytotoxic chemotherapy) in management of advanced melanoma that is both unresectable and carries the BRAF V500E mutation.
2. Both vemurafenib and dabrafenib is most commonly used in treatment of thyroid carcinoma and non-small cell lung cancer.
3. Both
4. Neither
Dabrafenib plus trametinib:
1. Useful in treating patients with advanced or metastatic anaplastic thyroid cancer.
2. This combination treatment yielded an overall response rate of about 70% anyone-year median duration of response of about 90%.
3. Both
4. Neither
Dabrafenib pharmacokinetics/pharmacodynamics:
1. Terminal half-life for dabrafenib is about 8 hours after oral administration.
2. Dabrafenib is metabolized by the cytochrome P450 drug metabolizing system, mainly by the CYP3A4 and CYP2C8 isoforms
3. Both
4. Neither
Resistance to dabrafenib:
1. As monotherapy, dabrafenib may exhibit therapeutic resistance after about six months of administration.
2. Dabrafenib, in combination with trametinib, Results in a delay of drug resistance development.
3. Both
4. Neither
BRAF inhibitors used in treating melanoma can induce dermatologic cancer, including squamous cell carcinoma.
1. True
2. False
Most common adverse effects associated with dabrafenib administration:
1. Hyperkeratosis
2. Pyrexia
3. Arthralgia
4. Papilloma
Common adverse effect(s) when dabrafenib is administered in combination with trametinib
1. Pyrexia
2. Rash
3. Chills
4. A & B
5. B & C
6. A & C
7. A, B & C