Buparlisib

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Buparlisib[edit | edit source]

Chemical structure of Buparlisib

Buparlisib is an investigational drug that acts as a pan-class I phosphoinositide 3-kinase (PI3K) inhibitor. It is primarily being studied for its potential use in the treatment of various types of cancer.

Mechanism of Action[edit | edit source]

Buparlisib works by inhibiting the activity of the PI3K enzyme, which is part of the PI3K/AKT/mTOR pathway. This pathway is crucial for regulating cell growth, proliferation, and survival. In many cancers, this pathway is dysregulated, leading to uncontrolled cell growth and survival. By inhibiting PI3K, buparlisib aims to restore normal cell cycle control and induce apoptosis in cancer cells.

Clinical Development[edit | edit source]

Buparlisib has been evaluated in several clinical trials for its efficacy and safety in treating different types of cancer, including breast cancer, lung cancer, and glioblastoma. It is often studied in combination with other therapies to enhance its anticancer effects.

Breast Cancer[edit | edit source]

In breast cancer, particularly in hormone receptor-positive, HER2-negative subtypes, buparlisib has been investigated in combination with endocrine therapy. The rationale is to overcome resistance to endocrine therapy by targeting the PI3K pathway.

Glioblastoma[edit | edit source]

Glioblastoma, a highly aggressive form of brain cancer, has also been a target for buparlisib studies. The drug's ability to cross the blood-brain barrier makes it a candidate for treating brain tumors.

Side Effects[edit | edit source]

Common side effects of buparlisib include hyperglycemia, rash, and diarrhea. Due to its mechanism of action, it can also affect normal cells, leading to adverse effects such as fatigue and nausea.

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Contributors: Prab R. Tumpati, MD