Drug intelligence / Profile preview

PD180970

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intperitoneal
01

Overview

PD180970 is a potent, ATP-competitive small molecule tyrosine kinase inhibitor belonging to the pyrido[2,3-d]pyrimidine class. It primarily targets the Bcr-Abl (c-Abl) and Src family kinases (SFKs), including Src, Fyn, and Yes, as well as the c-Kit receptor tyrosine kinase. Originally identified as a Bcr-Abl inhibitor for the treatment of chronic myeloid leukemia (CML), PD180970 has demonstrated activity against several imatinib-resistant Bcr-Abl mutations. Beyond oncology, it is being investigated for neurodegenerative disorders such as Parkinson's disease, where it acts by inhibiting c-Abl to reduce α-synuclein pathology, induce mTOR-independent autophagy, and suppress neuroinflammation. In preclinical models of prostate cancer, it has been shown to regulate AR-V7 expression and inhibit androgen-independent growth.

02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)FYN (Proto-oncogene tyrosine-protein kinase Fyn)YES1 (YES proto-oncogene 1 tyrosine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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