PIPELINE
Nuvation Bio is focused on treating patients with the most difficult-to-treat cancers for which conventional therapies have failed. We are advancing multiple compounds that have been generated from our drug discovery and development programs, which include a clinical stage bromodomain and extra-terminal (BET) inhibitor program and a novel, small molecule drug-drug conjugate (DDC) platform that to date has yielded investigational candidates targeting solid tumors.
Program
potential indication(s)
Current Stage
preclinical
phase 1
Phase 2
Phase 3
ANTICIPATED MILESTONES &
RECENT UPDATES
Advanced
solid tumors
NUV-868
Enrollment ongoing in Phase 1 dose escalation
NUV-868
(BET)
Ovarian, TNBC,
pancreatic, mCRPC &
other solid tumors
NUV-868 +
olaparib
Enrollment ongoing in Phase 1b dose escalation
mCRPC
NUV-868 +
enzalutamide
Enrollment ongoing in Phase 1b dose escalation
Drug-Drug
Conjugate
Platform
Solid tumors
Clinical candidate selected; submit IND filing by year end 2023
BET: Bromodomain and extra-terminal motif proteins; mCRPC: Metastatic castration-resistant prostate cancer; IND: Investigational New Drug; TNBC: Triple-negative breast cancer.
BET
NUV-868, a BD2-selective oral small molecule bromodomain and extra-terminal (BET) inhibitor, inhibits BRD4. BRD4 is a key member of the BET family, which epigenetically regulates proteins that control tumor growth and differentiation.
NUV-868 is almost 1,500 times more selective for BD2 than BD1 and is designed to alleviate the therapeutic limiting toxicities observed by other non-BD2 selective BET inhibitors. NUV-868 in combination with androgen-receptor directed therapies may help to overcome resistance in prostate cancer. In addition, NUV-868 in combination with PARP inhibitors may act synergistically to increase efficacy across multiple solid tumors.
We initiated a Phase 1 monotherapy, dose escalation study of NUV-868 for the treatment of patients with advanced solid tumors. In addition, we initiated a Phase 1b dose escalation study of NUV-868 in combination with olaparib for patients with ovarian, pancreatic, metastatic castration-resistant prostate, triple negative breast cancers and other solid tumors, and of NUV-868 in combination with enzalutamide for patients with metastatic castration-resistant prostate cancer. Enrollment is currently ongoing in the Phase 1 monotherapy and Phase 1b combination studies.
NUV-868, a BD2-selective oral small molecule bromodomain and extra-terminal (BET) inhibitor, inhibits BRD4. BRD4 is a key member of the BET family, which epigenetically regulates proteins that control tumor growth and differentiation.
NUV-868 is almost 1,500 times more selective for BD2 than BD1 and is designed to alleviate the therapeutic limiting toxicities observed by other non-BD2 selective BET inhibitors. NUV-868 in combination with androgen-receptor directed therapies may help to overcome resistance in prostate cancer. In addition, NUV-868 in combination with PARP inhibitors may act synergistically to increase efficacy across multiple solid tumors.
In March 2022, we initiated a Phase 1 monotherapy dose escalation study of NUV-868 in patients with advanced solid tumors. In December 2022, we initiated a Phase 1b dose escalation study of NUV-868 in combination with olaparib in patients with ovarian cancer, pancreatic cancer, metastatic castration-resistant prostate cancer (mCRPC), triple negative breast cancer, and other solid tumors, and in combination with enzalutamide in patients with mCRPC. Enrollment remains ongoing in both the Phase 1 and Phase 1b studies.
DDC Platform
Our proprietary, small molecule Drug-Drug Conjugate (DDC) platform leverages a novel therapeutic approach within the drug-conjugate class of anti-cancer therapies. The platform is designed to selectively deliver potent anti-cancer therapeutics to cancer cells to exert greater toxicity against these target tumor cells than against healthy non-target tissues.
Utilizing this platform, we are able to conjugate tissue-selective, targeted small molecules with anti-tumor agents to create unique therapeutic candidates. We believe our DDC technology will be broadly applicable and can be replicated across many existing therapies to transform the standard-of-care in multiple oncology indications.
We selected the first clinical candidate from our DDC platform in 2022 and plan to submit an IND filing for this candidate by the end of 2023.
Our proprietary, small molecule Drug-Drug Conjugate (DDC) platform leverages a novel therapeutic approach within the drug-conjugate class of anti-cancer therapies. The platform is designed to selectively deliver potent anti-cancer therapeutics to cancer cells to exert greater toxicity against these target tumor cells than against healthy non-target tissues.
Utilizing this platform, we are able to conjugate tissue-selective, targeted small molecules with anti-tumor agents to create unique therapeutic candidates. We believe our DDC technology will be broadly applicable and can be replicated across many existing therapies to transform the standard-of-care in multiple oncology indications.
In 2022, we nominated an undisclosed DDC as the first clinical candidate from our DDC platform. We expect to submit an Investigational New Drug (IND) application for this candidate with the U.S. Food and Drug Administration by year end 2023.
