Xevinapant

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Overview of the drug Xevinapant


{{Drugbox | verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (2S)-2-[[4-[[2-(3,5-difluorophenyl)acetyl]amino]phenyl]methyl]-1-[(2S)-2-[[4-[[2-(3,5-difluorophenyl)acetyl]amino]phenyl]methyl]pyrrolidine-1-carbonyl]pyrrolidine-2-carboxylic acid | image = Xevinapant.svg | image2 = }}

Xevinapant is a small molecule inhibitor of inhibitor of apoptosis proteins (IAPs), which are proteins that prevent apoptosis, or programmed cell death. It is being investigated for its potential use in the treatment of various types of cancer, particularly head and neck squamous cell carcinoma (HNSCC).

Mechanism of Action[edit | edit source]

Xevinapant functions by targeting and inhibiting IAPs, specifically the cellular IAPs (cIAP1 and cIAP2) and X-linked IAP (XIAP). These proteins are often overexpressed in cancer cells, allowing them to evade apoptosis and continue proliferating. By inhibiting these proteins, Xevinapant promotes the activation of caspases, which are enzymes that play a crucial role in the execution phase of cell apoptosis. This leads to the induction of cell death in cancer cells.

Clinical Development[edit | edit source]

Xevinapant is currently undergoing clinical trials to evaluate its efficacy and safety in combination with other therapies. It has shown promise in early-phase trials, particularly when used in conjunction with chemoradiotherapy for the treatment of locally advanced HNSCC. The drug is administered orally and has been well-tolerated in clinical settings, with manageable side effects.

Potential Applications[edit | edit source]

While the primary focus of Xevinapant's development has been on HNSCC, its mechanism of action suggests potential applicability in other cancers where IAPs are implicated in disease progression. Research is ongoing to explore its use in other solid tumors and hematological malignancies.

Side Effects[edit | edit source]

The side effects of Xevinapant observed in clinical trials include fatigue, nausea, and hematological abnormalities such as neutropenia and anemia. These side effects are generally consistent with those seen in other cancer therapies and are considered manageable with appropriate supportive care.

Future Directions[edit | edit source]

The future of Xevinapant in cancer therapy looks promising, with ongoing studies aimed at optimizing its use in combination with other therapeutic agents. Researchers are also investigating biomarkers that could predict response to Xevinapant, which would help in personalizing treatment for patients.

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Contributors: Prab R. Tumpati, MD