Clinical trials
Follow clinical development from study design and recruitment through results.
- Trial phase
- Status
- Readouts
Drug intelligence / Profile preview
CGP62221
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral (as A Metabolite Of Midostaurin)
01
Overview
CGP62221 is an active **O-demethylated metabolite** of the oral multi-targeted kinase inhibitor midostaurin. Midostaurin is metabolized primarily by hepatic CYP3A4 to produce CGP62221, which retains pharmacologic activity. While CGP62221 specifically blocks c-kit-dependent mast cell proliferation and inhibits IgE-mediated histamine release, it is also implicated in broad spectrum inhibition of kinase signaling pathways *in vitro*. The metabolite exhibits a markedly prolonged elimination half-life and is >99.8% bound to plasma proteins, mostly α1-acid glycoprotein. CGP62221 is under investigation as part of midostaurin therapy for malignancies such as acute myeloid leukemia and systemic mastocytosis[1][2][4][5].
- Other names
- O-demethylated midostaurin
02
Targets
FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)LYN (LYN proto-oncogene, Src family tyrosine kinase)PDGFR (PDGFR family)PDK (Pyruvate dehydrogenase kinase isoform 1)PRKCA (Protein kinase C alpha)RET (Rearranged during transfection receptor tyrosine kinase)SYK (Spleen Tyrosine Kinase)NTRK1 (Tropomyosin-related receptor kinase A)VEGFR2 (Vascular endothelial growth factor receptor 2)
Beyond the preview
Go deeper on CGP62221.
Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.
Indications & development
Explore development by indication, patient population, and geography.
- Indications
- Development status
- Countries
Licensing & deals
Trace asset ownership, licensing agreements, and commercial partnerships.
- Partners
- Deal terms
- Milestones
Patents & exclusivity
Explore the patent landscape and regulatory exclusivity around an asset.
- Patents
- Expiration dates
- Exclusivity
Competitive landscape
Compare development programs by target, modality, and indication.
- Competing assets
- Targets
- Development stage
Research & analysis
Connect source evidence and development news to your research questions.
- Publications
- News
- Analysis
Bring the full picture into focus.
See how Gosset can support your research on CGP62221.