Vemurafenib

Vemurafenib was developed by Roche and obtained FDA approval for marketing in the United States in 2011.

Before using Vimafenib, doctors need to conduct a comprehensive health assessment of patients and inform them of possible side effects and monitoring methods.

Vemurafenib is an oral small molecule inhibitor targeting BRAF V600 mutant tumors, which has significant anti-tumor efficacy. However, attention should also be paid to its possible side effects and safety issues during use.

1.Main components

Vemurafenib

2. Adapt to the population

Adult patients with Melanoma and Erdheim Chester Disease.

3.Medication for special populations

3.1Pregnant

Based on its mechanism of action, Vemurafenib can cause fetal harm when administered to a pregnant  woman. There are no available data on the use of Vemurafenib in  pregnant women to determine the drug-associated risk; however, placental transfer of vemurafenib to a fetus  has been reported. Exposure to vemurafenib could not be achieved in animals at levels sufficient to fully  address its potential toxicity in pregnant women. Advise pregnant women of the potential harm to a fetus.

3.2Lactation

There is no information available regarding the presence of vemurafenib in human milk, effects on the  breastfed infant, or effects on milk production. Because of the potential for serious adverse reactions in a  breastfed infant, including malignancy, severe dermatologic reactions, QT prolongation, hepatotoxicity,  photosensitivity, and ophthalmologic toxicity, advise women not to  breastfeed during treatment with Vemurafenib and for 2 weeks after the final dose.

3.3Females and Males of Reproductive Potential

Based on its mechanism of action, Vemurafenib can cause fetal harm when administered to a pregnant  woman. Advise females of reproductive potential to use effective  contraception during treatment with Vemurafenib and for 2 weeks after the final dose.

3.4 Pediatric Use

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

3.5 Geriatric Use

Clinical studies of Vemurafenib did not include sufficient numbers of subjects aged 65 and over to determine  whether they respond differently from younger subjects.

3.6 Renal Impairment

No formal clinical study has been conducted to evaluate the effect of hepatic impairment on the  pharmacokinetics of vemurafenib. No dose adjustment is recommended for patients with mild and moderate  hepatic impairment based on a population pharmacokinetic analysis. The  appropriate dose of Vemurafenib has not been established in patients with severe hepatic impairment.

3.7Hepatic Impairment

No formal clinical study has been conducted to evaluate the effect of hepatic impairment on the  pharmacokinetics of vemurafenib. No dose adjustment is recommended for patients with mild and moderate  hepatic impairment based on a population pharmacokinetic analysis. The  appropriate dose of Vemurafenib has not been established in patients with severe hepatic impairment.

4.Drug overdose

There is no information on overdosage of Vemurafenib.

5. Drug storage

Store at room temperature 20°C–25°C (68°F–77°F); excursions permitted between  15°C and 30°C (59°F and 86°F), See USP Controlled Room Temperature. Store in the original container with  the lid tightly closed.

6.Pharmacokinetics

The mean bioavailability of vemurafenib at steady state was 64% (56% CV). The median time to reach  maximum plasma vemurafenib concentration (Tmax) was 3 hours following multiple doses.

from FDA，2020.12