Drug intelligence / Profile preview

uzansertib

Development stage
Unknown
Lead developer
Incyte
Modality
Small Molecules
Administration
Oral
01

Overview

Uzansertib is an orally administered, selective, ATP-competitive pan-PIM serine/threonine kinase inhibitor developed by Incyte. It inhibits PIM1, PIM2, and PIM3, suppressing phosphorylation of downstream substrates involved in malignant-cell survival and proliferation. In the Medical College of Wisconsin phase Ib study, uzansertib was evaluated with pomalidomide and dexamethasone for relapsed and/or refractory multiple myeloma. ([guidetopharmacology.org](https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10626&tab=refs))

Other names
INCB-053914INCB053914INCB 053914
02

Targets

PIM1 (Proviral integration site for moloney murine leukemia virus kinase 1)PIM3 (Proviral integration site for Moloney murine leukemia virus kinase 3)RPS6KA3 (RSK2)PIM2 (Proto-oncogene serine/threonine-protein kinase Pim2)PASK (Per-arnt-sim kinase)

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