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 clinical candidate from our novel, small molecule drug-drug conjugate (DDC) platform.
Program
potential indication(s)
Current Stage
preclinical
phase 1
Phase 2
Phase 3
ANTICIPATED MILESTONES &
RECENT UPDATES
Advanced
solid tumors
NUV-868
Treatment ongoing in Phase 1 dose escalation
NUV-868
(BET)
Ovarian, TNBC,
pancreatic, mCRPC
& other solid
tumors
NUV-868 +
olaparib
Treatment ongoing in Phase 1b dose escalation
mCRPC
NUV-868 +
enzalutamide
Treatment ongoing in Phase 1b dose escalation
NUV-1511
(DDC)
Advanced solid tumors (post-Enhertu
and/or post-Trodelvy progression),
HER2- mBC, mCRPC, pancreatic & PROC
IND clearance; Initiate Phase 1/2 study in 1H 2024

BET: Bromodomain and extra-terminal motif proteins; DDC: Drug-drug conjugate; HER2- mBC: Human epidermal growth factor receptor 2-negative metastatic breast cancer; IND: Investigational New Drug; mCRPC: Metastatic castration-resistant prostate cancer; PROC: platinum-resistant ovarian cancer; 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. Treatment 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 2024, we announced that the U.S. Food and Drug Administration has cleared an Investigational New Drug (IND) application for NUV-1511, the first clinical candidate from our DDC platform. We anticipate initiating a Phase 1/2 clinical study of NUV-1511 in the first half of 2024 that will initially evaluate safety and tolerability, and explore the potential for clinical efficacy, in patients with advanced solid tumors who previously received and progressed on or after treatment with Enhertu® and/or Trodelvy® per approved FDA labeling, human epidermal growth factor receptor 2-negative (HER2-) metastatic breast cancer, metastatic castration-resistant prostate cancer (mCRPC), pancreatic cancer, and platinum-resistant ovarian cancer (PROC).