ADDED
Our clinical stage product candidates include: Rinzimetostat (formerly ORIC-944), an allosteric inhibitor of the polycomb repressive complex 2 (PRC2) via the embryonic ectoderm development (EED) subunit, for which we licensed development and commercialization rights from Mirati Therapeutics, Inc.
(Mirati) under a license agreement (Mirati License Agreement).
We filed and cleared an Investigational New Drug application (IND) with the Food and Drug Administration (FDA) for rinzimetostat in the fourth quarter of 2021.
We also announced that we entered into clinical trial collaboration and supply agreements with Janssen Research Development, LLC, a Johnson and Johnson company (Johnson Johnson) and Bayer Consumer Care AG (Bayer), to evaluate rinzimetostat in combination with Erleada (apalutamide), Johnson Johnson s androgen receptor (AR) inhibitor, and Nubeqa (darolutamide), Bayer s AR inhibitor.
In November 2025, we announced the completion of the dose exploration portion of the Phase 1b trial and the selection of provisional recommended Phase 2 doses (RP2Ds) of rinzimetostat to be tested in combination with the approved doses of darolutamide and apalutamide in the dose optimization portion of the Phase 1b trial: 400 mg and 600 mg QD of rinzimetostat in combination with 600 mg BID of darolutamide; and 600 mg, 800 mg and 1,200 mg QD of rinzimetostat in combination with 240 mg QD of apalutamide.
Also, in November 2025, we reported Phase 1b dose exploration data in 20 patients with mCRPC, who were treated with rinzimetostat in combination with 240 mg QD of apalutamide or with 600 mg BID of darolutamide.
The November 2025 data set (cutoff date of September 22, 2025) demonstrated PSA responses and circulating tumor DNA (ctDNA) reductions across all rinzimetostat dose levels and at comparable rates in combination with apalutamide or with darolutamide.
Broad and deep PSA responses were demonstrated, with 55% of patients achieving a PSA50 response rate (confirmed in 40%), and 20% of patients achieving a PSA90 response rate (all confirmed).
Rapid and deep ctDNA responses were observed in patients across a breadth of AR mutations and other gene alterations, with 76% of patients achieving greater than 50% ctDNA reduction, and 59% of patients achieving ctDNA clearance.
Both combination regimens demonstrated a safety profile compatible with long-term dosing, with the vast majority of treatment-related adverse events (TRAEs) Grade 1 or 2 in severity and consistent with PRC2 and AR inhibition.
REMOVED
Our clinical stage product candidates include: ORIC-114, a brain penetrant, orally bioavailable, irreversible inhibitor that selectively targets epidermal growth factor receptor (EGFR) exon 20, human epidermal growth factor receptor 2 (HER2) exon 20 and EGFR atypical mutations, for which we licensed development and commercialization rights from Voronoi Inc.
We also filed and cleared an Investigational New Drug Application (IND) with the U.S.
Food and Drug Administration (FDA) for ORIC-114 in the third quarter of 2022.
We are enrolling a Phase 1b trial of ORIC-114 as a single-agent, in patients with advanced solid tumors with EGFR and HER2 exon 20 insertion mutations, EGFR atypical mutations or HER2 amplifications, which allows enrollment of patients with CNS metastases that are either treated or untreated but asymptomatic.
We reported initial Phase 1b data from this trial at the European Society for Medical Oncology (ESMO) Congress in October 2023, which demonstrated both systemic and intracranial activity across multiple dose levels in a heavily pre-treated patient population.
In April 2024, we announced the selection of two provisional recommended Phase 2 dose (RP2D) levels of ORIC-114 at 80 mg and 120 mg daily (QD), which are being further evaluated in three dose expansion cohorts for dose optimization and final RP2D selection.
These expansion cohorts have now been initiated in patients with second-line non-small cell lung cancer (NSCLC) with EGFR exon 20 insertion mutations (EGFR exon 20 inhibitor-na ve), HER2 exon 20 insertion mutations, or EGFR atypical mutations.
We expect to report updated Phase 1b data for the 2L EGFR exon 20 and 2L+ HER2 exon 20 cohorts in the first half of 2025 and the 2L+ EGFR atypical cohort in the second half of 2025.
We also initiated cohorts for the treatment of patients with first-line, treatment-na ve NSCLC EGFR exon20 insertion mutations and first-line, treatment-na ve NSCLC EGFR atypical mutations, and expect to report Phase 1b data in the first half of 2026 and mid-2026, respectively.
In January 2025, we announced that we entered into a clinical trial and supply agreement with Janssen Research Development, LLC, a Johnson and Johnson company (Johnson Johnson), to evaluate ORIC-114 in combination with subcutaneous (SC) amivantamab for the first line treatment of patients with advanced NSCLC with EGFR exon 20 insertion mutations, and we initiated a Phase 1b trial in the first quarter of 2025 and expect to report Phase 1b data in mid-2026.