March 2017March 2017
New Product - Venclexta
Venclexta (venetoclax) is an orally bioavailable small molecule inhibitor of BCL-2, an anti-apoptotic protein. Overexpression of BCL-2 has been demonstrated in chronic lymphocytic leukaemia (CLL) cells and has been implicated in resistance to certain therapeutic agents. Venetoclax helps restore the process of apoptosis by binding directly to the BCL-2 protein, displacing pro-apoptotic proteins like BIM, triggering mitochondrial outer membrane permeabilisation, the release of cytochrome c from mitochondria and the activation of caspases. In nonclinical studies, venetoclax demonstrated cytotoxic activity in tumour cells that overexpress BCL-2. Venclexta is indicated for the treatment of patients with relapsed or refractory CLL with 17p deletion, or patients with relapsed or refractory CLL for whom there are no other suitable treatment options. (Note to indications: the indications are approved based on overall response rates. Duration of response and improvements in overall survival, progression free survival or health related quality of life have not been established.) Concomitant use of Venclexta with strong CYP3A inhibitors at initiation and during the dose titration phase is contraindicated. Venclexta is available as a 4 week starter pack consisting of week 1 (14 x 10 mg tablets), week 2 (7 x 50 mg tablets), week 3 (7 x 100 mg tablets) and week 4 (14 x 100 mg tablets). Venclexta is also available as 10 mg tablets in a pack of 14’s, 50 mg tablets in a pack of 7’s and 100 mg tablets in a pack of 120’s.
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