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Deciphera's kinase switch inhibitors target the mechanisms that render kinases oncogenic, retain potency against gatekeeper mutations, and afford selectivity profiles not easily attained by other approaches.

BCR-ABL Program

Chronic Myelogeous Leukemia (CML) program

DCC-2036

DCC-2036 inhibits BCR-ABL kinase, an oncogenic fusion protein kinase resulting from chromosomal translocation (Philadelphia + chromosome). BCR-ABL is causative of myeloproliferative diseases, including chronic myelogenous leukemia (CML).

Late-stage preclinical development

  • Phase 1 trials in CML scheduled for Q1 2009.
      » Inhibitor of BCR-ABL and T315I BCR-ABL gatekeeper mutant kinases

  • Treatment of accelerated/blast crisis CML.
      » DCC-2036 inhibits SRC-like kinases LYN, HCK, FGR
  • Treatment of other myeloproliferative diseases and solid tumors.
      » DCC-2036 inhibits TIE2 and KDR kinases, contributing an anti-angiogensis component to its mechanism

In preclinical studies, DCC-2036 has demonstrated potent enzymatic and cellular inhibition of BCR-ABL, the T315I gatekeeper mutant, and other clinically relevant P-loop & Activation loop mutants. DCC-2036 is highly efficacious in animal models of human T315I CML. DCC-2036 is being developed as an orally administered treatment for CML.



DCC-2157

DCC-2157 inhibits BCR-ABL kinase, an oncogenic fusion protein kinase resulting from chromosomal translocation (Philadelphia + chromosome). BCR-ABL is causative of myeloproliferative diseases, including chronic myelogenous leukemia (CML).

CML candidate- preclinical development

  • Treatment of chronic phase CML.
      » Inhibitor of BCR-ABL and T315I BCR-ABL gatekeeper mutant kinases
  • Treatment of solid tumors.
      » DCC-2157 inhibits cKIT, PDGFR-alpha and KDR kinases
      » Provides a profile for the treatment of primary GIST and other solid tumors

In preclinical studies, DCC-2157 has demonstrated potent enzymatic and cellular inhibition of BCR-ABL, the T315I gatekeeper mutant, and other clinically relevant P-loop & Activation loop mutants. DCC-2157 is highly efficacious in animal models of human T315I CML. DCC-2157 is being developed as an orally administered treatment for CML.

 


Deciphera Pharmaceuticals, LLC
4950 Research Park Way
Lawrence, KS 66047

785-838-3767 phone
785-838-3747 fax
info@deciphera.com

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