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dasatinib + lomustine
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Dasatinib + lomustine is an investigational combination of two small molecule chemotherapeutic agents used in clinical trials for the treatment of recurrent glioblastoma and other brain tumors. Dasatinib is a multi-targeted tyrosine kinase inhibitor that blocks several kinases involved in tumor growth and survival, including BCR-ABL, SRC family kinases, c-KIT, EPHA2, and PDGFR. Lomustine (CCNU) is an alkylating agent of the nitrosourea class that exerts its antitumor effect by cross-linking DNA and RNA strands to inhibit cancer cell replication. The combination has been studied primarily for recurrent glioblastoma but was found to have significant hematological toxicity with suboptimal exposure to both drugs[3]. This regimen remains experimental.
- Other names
- CCNU
02
Targets
ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)DNAEPHA2 (Ephrin type-A receptor 2)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)SFK (SRC family kinases)
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