Defactinib

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Defactinib

Defactinib is a small molecule inhibitor primarily focused on the treatment of cancer. It targets the focal adhesion kinase (FAK), a protein kinase that is often overexpressed in several types of tumors and plays a crucial role in cancer cell survival and metastasis. By inhibiting FAK, defactinib aims to disrupt cancer cell growth and spread, making it a potential therapeutic option for various cancers.

Mechanism of Action[edit | edit source]

Defactinib works by selectively inhibiting the activity of focal adhesion kinase (FAK), a non-receptor tyrosine kinase. FAK is involved in signaling pathways that regulate cancer cell proliferation, survival, and migration. In many cancers, FAK is overexpressed or hyperactivated, contributing to tumor growth and metastasis. By blocking FAK's activity, defactinib can interfere with these critical cancer cell processes, potentially leading to reduced tumor growth and spread.

Clinical Trials[edit | edit source]

Defactinib has been evaluated in several clinical trials for its efficacy and safety in treating various types of cancer, including mesothelioma, non-small cell lung cancer (NSCLC), and pancreatic cancer. These studies have explored defactinib as both a monotherapy and in combination with other cancer treatments, such as chemotherapy and immunotherapy. The outcomes of these trials are crucial for determining the potential role of defactinib in cancer therapy.

Safety and Efficacy[edit | edit source]

The safety and efficacy of defactinib are determined through rigorous clinical trials. Common side effects reported in these studies include fatigue, nausea, and diarrhea, which are generally consistent with those observed for other cancer therapies. The efficacy of defactinib varies depending on the type of cancer and the specific characteristics of the tumor. Ongoing research aims to identify biomarkers that can predict which patients are most likely to benefit from defactinib treatment.

Future Directions[edit | edit source]

Research on defactinib continues to evolve, with ongoing studies investigating its use in various cancer types and in combination with other therapeutic agents. The identification of patient subgroups that may benefit most from defactinib treatment is a key area of focus. Additionally, understanding the mechanisms of resistance to FAK inhibition will be important for optimizing the use of defactinib in cancer therapy.


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Contributors: Prab R. Tumpati, MD