OPN-6602

dual EP300/CBP inhibitor

Target

Hit identification

Lead optimization

Preclinical

Phase 1

Phase 2

Target:

EP300/CBP

icon

Therapeutic area:

multiple myeloma

icon

Value:

best-in-class potential,
potent and selective

icon

Safety:

favorable 28-day safety profiles
in mouse and dog studies

icon

Next milestone:

recommended Phase 2
dose as single agent

OPN-6602 regulates gene transcription via chromatin remodeling

E1A binding protein p300 (EP300) and CREB-binding protein (CBP) are paralog histone acetyltransferases (HAT) bearing bromodomains that are involved in transcription and cell growth, survival, apoptosis and DNA repair. EP300/CBP are master regulators of oncogenic signaling and immune evasion.

diagram

Inhibition of EP300/CBP bromodomains blocks HAT activity, reducing gene expression and tumor growth, potentially delaying or preventing tumor growth and drug resistance.

OPN-6602 is a potent and selective EP300/CBP bromodomain inhibitor. OPN-6602 blocks signaling involved in cell growth and tumorigenesis by modulation of histone acetylation and the recruitment of EP300/CBP bromodomains.

diagram

OPN-6602 reduces androgen receptor (AR)-driven and MYC gene expression while acting through a distinct mechanism from BET bromodomain inhibitors. Inhibition of AR signaling with OPN-6602 has been shown to reduce tumor growth in metastatic castration resistant prostate cancer (mCRPC) xenograft and PDX models.

Interferon regulatory factor 4 (IRF4) is a highly expressed transcription factor responsible for regulating lymphocyte differentiation, and is overexpressed in multiple myelomas. OPN-6602 downregulates IRF4/MYC through EP300/CBP inhibition. OPN-6602 shows differentiated potency and efficacy in multiple myeloma xenograft models. As an epigenetic modulator, OPN-6602 has potential therapeutic benefit across numerous indications.

Clinical trials

OPN-6602 is currently being tested in patients with relapsed and/or refractory multiple myeloma as a single agent and later in combination with other therapies.

To learn more about this trial, please click below.

LEARN MORE