Dabrafenib

Dabrafenib is a potent and selective BRAF inhibitor, available in two drug sizes of 50mg and 75mg.

On May 29, 2013, the US Food and Drug Administration approved Dabrafenik for the treatment of metastatic melanoma and inoperable melanoma. On June 22, 2017, the US Food and Drug Administration expanded the indications for Dabrafenib.

Dabrafenib is a BRAF inhibitor that can specifically block the activity of BRAF proteins, inhibit tumor cell proliferation and survival.

1.Main components

Dabrafenib

2.Adapt to the population

BRAF V600 mutation positive patients with unresectable or metastatic melanoma.

3.Medication for special populations

3.1Pregnancy

Based on its mechanism of action, Dabrafenib can cause fetal harm when administered to a pregnant woman. If this drug is used during pregnancy or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to a fetus. 

3.2Nursing Mothers

It is not known whether this drug is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions from Dabrafenib in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

3.3Pediatric Use

The safety and effectiveness of Dabrafenib have not been established in pediatric patients.

3.4Geriatric Use

One hundred and twenty-six (22%) of 586 patients in clinical trials of Dabrafenib and 40 (21%) of the 187 patients receiving Dabrafenib in Trial 1 were ≥65 years of age. No overall differences in the effectiveness or safety of Dabrafenib were observed in the elderly in Trial 1.

3.5Females and Males of Reproductive Potential

Advise female patients to use highly effective contraception during treatment and for 4 weeks following discontinuation of treatment.

Advise male patients of potential risk for impaired spermatogenesis.

3.6Hepatic Impairment

Dose adjustment is not recommended for patients with mild hepatic impairment.An appropriate dose has not been established for patients with moderate to severe hepatic impairment. 

3.7Renal Impairment

Dose adjustment is not recommended for patients with mild or moderate renal impairment. An appropriate dose has not been established for patients with severe renal impairment. 

4.Drug overdose

Drug overdose is not yet clear.

5.Drug storage

Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F). 

6.Pharmacokinetics

After oral administration, median time to achieve peak plasma concentration (Tmax)is 2 hours. 

from FDA,2013.05