Drug intelligence / Profile preview

OPN-6602 + dexamethasone

Development stage
Unknown
Lead developer
Opna Bio
Modality
Small Molecules
Administration
Oral
01

Overview

OPN-6602 + dexamethasone is an investigational, orally administered combination therapy under clinical evaluation for the treatment of relapsed and/or refractory multiple myeloma. OPN-6602 is a potent and selective small molecule inhibitor of the EP300 and CREB-binding protein (CBP) bromodomains. By inhibiting EP300/CBP, OPN-6602 downregulates IRF4 and MYC expression, critical transcription factors for multiple myeloma cell survival and proliferation[2][3][4][5]. Dexamethasone, a synthetic glucocorticoid, is commonly used in multiple myeloma regimens for its anti-inflammatory and lympholytic effects, functioning via activation of the glucocorticoid receptor and subsequent suppression of cytokine signaling (notably interleukin-6)[1]. Preclinical studies demonstrate that OPN-6602 exhibits significant anti-tumor activity as monotherapy and shows synergistic effects when combined with dexamethasone[2][5]. Clinical trials are ongoing to evaluate safety, tolerability, pharmacokinetics, and preliminary antitumor efficacy in patients with relapsed/refractory multiple myeloma[2][3][4][5].

02

Targets

EP300 (Histone acetyltransferase p300)GR (Glucocorticoid receptor)CREBBP BD (Creb-binding protein bromodomain)

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