Crenolanib

Overview

Crenolanib is a small molecule tyrosine kinase inhibitor that targets the platelet-derived growth factor receptor (PDGFR) and the FMS-like tyrosine kinase 3 (FLT3). It is primarily investigated for its potential use in treating various types of cancer, including acute myeloid leukemia (AML) and gastrointestinal stromal tumors (GISTs).

Mechanism of Action

Crenolanib functions by inhibiting the activity of PDGFR and FLT3, which are often overexpressed or mutated in certain cancers. By blocking these receptors, crenolanib can interfere with the signaling pathways that promote cancer cell proliferation and survival.

Clinical Applications

Acute Myeloid Leukemia

In acute myeloid leukemia, mutations in the FLT3 gene are common and are associated with poor prognosis. Crenolanib has shown promise in targeting these mutations, particularly the FLT3-ITD and FLT3-D835 mutations, which are resistant to other treatments.

Gastrointestinal Stromal Tumors

Crenolanib is also being studied for its efficacy in treating gastrointestinal stromal tumors, especially those that are resistant to other tyrosine kinase inhibitors like imatinib and sunitinib.

Pharmacokinetics

Crenolanib is administered orally and has a favorable pharmacokinetic profile, allowing it to be used in combination with other chemotherapeutic agents. Its ability to penetrate the central nervous system makes it a candidate for treating cancers with central nervous system involvement.

Side Effects

Common side effects of crenolanib include nausea, diarrhea, fatigue, and liver enzyme abnormalities. As with other tyrosine kinase inhibitors, careful monitoring of patients is necessary to manage these adverse effects.

Research and Development

Crenolanib is currently undergoing various clinical trials to evaluate its safety and efficacy in different cancer types. Ongoing research aims to optimize its use in combination therapies and to identify biomarkers that predict response to treatment.

Related Pages

• Tyrosine kinase inhibitor
• Acute myeloid leukemia
• Gastrointestinal stromal tumor
• Platelet-derived growth factor receptor
• FMS-like tyrosine kinase 3

Gallery

Chemical structure of Crenolanib