Instructions for Vemurafenib

1. Common name: Vemurafenib

Product name:Zelboraf, Zelboraf

All names: Vemurafenib tablets, Vemurafenib, Vemurafenib, Vemurafenib, Vemurafenib, Vemurafenib, Ripela

2. Indications:

1. Unresectable or metastatic melanoma: Vemurafenib is suitable for the treatment of patients with unresectable or metastatic melanoma whose BRAF V600E mutation is found by FDA-approved testing.

Restrictions on use: Vemurafenib is not indicated for the treatment of patients with wild-type BRAF melanoma

2. Erdheim-Chester disease (ECD): Vemurafenib is suitable for the treatment of patients with Erdheim-Chester disease who have BRAF V600 mutations.

3. Usage and dosage:

1. Before treatment: Before starting treatment with vemurafenib for patients with melanoma, doctors will confirm whether there is a BRAF V600E mutation in the melanoma specimen.

2. Recommended dose: The recommended dose of vemurafenib is 960 mg (four 240 mg tablets) orally every 12 hours, taken with or without food, and treatment continues until disease progression or unacceptable toxicity occurs. Missed doses can be taken up to 4 hours before the next dose.

3. Dosage adjustment: If adverse reactions occur after treatment with vemurafenib, the medication should be adjusted, interrupted or stopped under the guidance of a doctor.

Avoid concomitant use of strongCYP3A4 inducers during treatment with vemurafenib. If this cannot be avoided, increase the dose of vemurafenib by 240 mg (one tablet) based on tolerance. Two weeks after discontinuing the strong CYP3A4 inducer, resume the vemurafenib dose that was taken before starting the strong CYP3A4 inducer.

4. Adverse reactions:

Most common adverse reactions of any grade in patients treated with vemurafenib, in either study≥30%) for joint pain, rash, hair loss, fatigue, photosensitivity, nausea, pruritus, and skin papilloma. The most common (≥5%) Grade 3 adverse reactions were cutaneous squamous cell carcinoma and rash. After the marketing of vemurafenib, progression of pre-existing chronic myelomonocytic leukemia with NRAS mutations, benign, malignant, and unspecified tumors (including cysts and polyps), drug reactions with eosinophilia and systemic symptoms, neutropenia, pancreatitis, acute interstitial nephritis, acute tubular necrosis, Dupuytren's contracture, and plantar fascial fibromatosis have occurred.

5. Storage:

Vemurafenib is stored at room temperature20°C–25°C (68°F–77°F); excursions allowed between 15°C and 30°C (59°F and 86°F). Store in original container with lid tightly closed. Unused or expired medications should be used to minimize release of the drug into the environment. Pharmaceuticals should not be disposed of through wastewater and should be avoided through household waste.

6. Special groups:

1. Women: According to its mechanism of action, vemurafenib can cause harm to the fetus when used in pregnant women, including malignant tumors, severe skin reactions, QT interval prolongation, hepatotoxicity, photosensitivity and ophthalmic toxicity. Therefore, it is recommended that women of reproductive potential use effective contraception during treatment with vemurafenib and for 2 weeks after the last dose; women are advised not to breastfeed during treatment with vemurafenib and for 2 weeks after the last dose.

7. Mechanism of action:

Vemurafenib is a low molecular weight, oral inhibitor of mutant forms of BRAF serine-threonine kinase, including BRAF V600E. Vemurafenib also inhibits other in vitro kinases such as CRAF, ARAF, wild-type BRAF, SRMS, ACK1, MAP4K5, and FGR at similar concentrations. Some mutations in the BRAF gene, including V600E, result in constitutively activated BRAF protein, which can cause cell proliferation in the absence of growth factors required for normal proliferation. Vemurafenib has anti-tumor effects in BRAF V600E mutated melanoma cells and animal models.

Vemurafenib The original drug has been launched in China and has entered the scope of medical insurance. The price of 240mg*56 tablets per box may be around 7,000 yuan, which is very expensive. The Turkish version of Vemurafenib Original drug listed overseas, specifications240mg*56 tablets, may cost more than 2,000 yuan per box (the price may fluctuate due to exchange rates), which is relatively cheap. There is currently no generic version of Vemurafenib on the market. For more drug information and specific prices, please consult a medical consultant.