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newest 2010spec sheet8 rows
Bafetinib is an investigational second-generation tyrosine kinase inhibitor developed for Bcr-Abl-positive leukemias such as chronic myeloid leukemia (CML), designed to work against imatinib-resistant disease. It reached phase 2 clinical trials but was never approved.
- Showed activity against imatinib-resistant chronic myeloid leukemia in early trials
- Inhibits most common imatinib-resistant Bcr-Abl mutations
- Studied in CLL, prostate cancer, and brain tumor trials
Overview
A cancer drug candidate, not a nootropic; it's an antineoplastic kinase blocker that showed promise against imatinib-resistant leukemia but stalled in development.
Mechanism
Bafetinib is a dual inhibitor of the Bcr-Abl fusion kinase (the abnormal enzyme that drives chronic myeloid leukemia) and the Src-family kinase Lyn, which has been linked to imatinib resistance in CML. It was rationally designed from imatinib's chemical scaffold with modifications that improve binding potency; in preclinical studies it was 25 to 55-fold more potent than imatinib in vitro and at least 10-fold more potent in vivo. It inhibits 12 of the 13 most common imatinib-resistant Bcr-Abl point mutations, though it does not work against the T315I mutation. Bafetinib has also been shown to reverse multidrug resistance by inhibiting the drug-efflux transporters ABCB1 and ABCG2.
receptor fingerprint
Bcr-Abl fusion kinaseInhibitor
Lyn kinaseInhibitor
Safetyrisks and cautions, not medical advice
In phase 1 trials in imatinib-resistant or intolerant CML patients, bafetinib showed clinical activity, with major cytogenetic responses in about 19% of chronic-phase patients. A pilot phase 2 study in relapsed or refractory B-cell chronic lymphocytic leukemia found no treatment-limiting toxicity at a 240 mg twice-daily oral dose, though achieved blood concentrations were below levels needed to reliably kill CLL cells in preclinical models. It has also been studied in prostate cancer and brain tumor trials. Bafetinib has not been approved by any regulatory agency and is not commercially available.
Subjective profileweighing the evidence above
A well-designed successor to imatinib that showed activity in resistant leukemia and then stopped; blood levels in Phase 2 never reached what the preclinical work said was needed. Not approved, not available, and of interest now as drug-development history.
Resources
This entry is here for reference.
Research
- 1.Bafetinib, a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia
- 2.NS-187 (INNO-406), a Bcr-Abl/Lyn Dual Tyrosine Kinase Inhibitor
2 listed here; entry last updated July 2026
Reviews
My notesprivate to this device
FAQ
What is Bafetinib used for?
It was studied as a treatment for Bcr-Abl-positive leukemias, particularly imatinib-resistant chronic myeloid leukemia, and later for chronic lymphocytic leukemia and some solid tumors. It has not been approved for any use.
How does Bafetinib work?
It blocks the Bcr-Abl fusion kinase that drives CML, plus the Lyn kinase associated with resistance to older drugs like imatinib, shutting down the abnormal growth signals in leukemia cells.
Is Bafetinib well-researched?
It has a reasonable body of preclinical and early-phase clinical research, including phase 1 and pilot phase 2 trials, but development did not continue to approval.
Notes and cautions
- Achieved blood levels sometimes fell short of concentrations needed for effect in some cancers
- Does not work against the T315I resistance mutation
- Never approved or marketed; only available as a research chemical for lab use