PIPELINE
Nuvation Bio is focused on tackling some of the toughest challenges in cancer treatment. Our clinical trial programs include taletrectinib (ROS1 inhibitor), safusidenib (mIDH1 inhibitor), NUV-868 (BET inhibitor), and our Drug-Drug Conjugate (DDC) program.
Program
Therapeutic Area(s)
Current Stage of Development
Preclinical
Phase 1
Phase 2
Pivotal
Approved
Anticipated Milestones & Recent Updates
Taletrectinib1
(ROS1)
Advanced ROS1+ NSCLC
(treatment line agnostic)
• Approved by the U.S. FDA, Japan's MHLW, and China's NMPA
• Enrolling TRUST-IV study for early-stage ROS1+NSCLC
Safusidenib2
(mIDH1)
Diffuse IDH1-mutant glioma
• Entering pivotal study in high-grade IDH1-mutant glioma2
NUV-868
(BET)
Currently under internal evaluation
• Completed Phase 1 monotherapy and Phase 1b
combination studies in advanced solid tumors
Drug-drug conjugate
(DDC) Program
Solid tumors
• Currently evaluating preclinical candidates
NUV-868
(BET)
Advanced solid
tumors3
NUV-868 +
olaparib
Phase 1b dose escalation study ongoing
BET: Bromodomain and Extra-Terminal motif; ESMO: European Society of Medical Oncology Congress; MHLW: Ministry of Health, Labour and Welfare; mIDH1: mutant isocitrate dehydrogenase 1; NSCLC: Non-small cell lung cancer; ROS1+: c-ros oncogene 1-positive. 1. Worldwide development and commercial rights in-licensed from Daiichi Sankyo; rights to IBTROZI have been out-licensed in China (Innovent Biologics) and Japan (Nippon Kayaku). 2. Worldwide development and commercial rights in-licensed from Daiichi Sankyo, excluding Japan where Daiichi Sankyo retains development and commercial rights. Protocol amendment to upsize to a pivotal trial and include patients with grade 2 high-risk IDH1-mutant glioma are forthcoming.
ROS1
Taletrectinib is a highly selective, next-generation oral ROS1 tyrosine kinase inhibitor (TKI) designed to address some of the outstanding challenges of treating ROS1-positive (ROS1+) non-small cell lung cancer (NSCLC). For more information, visit the Our Medicine page.
Each year, more than one million people globally are diagnosed with NSCLC, the most common form of lung cancer. It is estimated that approximately 2% of people with NSCLC have ROS1+ disease. About 35% of people newly diagnosed with metastatic ROS1+ NSCLC have tumors that have spread to their brain. The brain is also the most common site of disease progression, with about 50% of previously treated patients developing central nervous system metastases. Despite recent progress for patients with ROS1+ NSCLC, there remains a need for treatment options that address some of the outstanding challenges of treating the disease.
mIDH1
Safusidenib is a novel, oral, potent, brain penetrant, targeted inhibitor of mutant IDH1 (mIDH1).
Safusidenib is being evaluated in a Phase 2 study for the treatment of patients with diffuse IDH1-mutant glioma. Safusidenib has shown high blood-brain barrier penetration in both pre-clinical and clinical studies and demonstrated anti-tumor activity and tolerability in a Phase 1 clinical study. Glioma is the most common type of adult brain cancer, and IDH1 mutations are present in the majority of low-grade diffuse gliomas.
BET
NUV-868 is a BD2-selective, oral, small molecule bromodomain and extra-terminal (BET) inhibitor that 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.
We have completed a Phase 1 monotherapy study and a Phase 1b study of NUV-868 in combination with olaparib or enzalutamide. We are evaluating next steps for the NUV-868 program, including further development in combination with approved products for indications in which BD2-selective BET inhibitors may improve outcomes for patients.
DDC
Our proprietary, small molecule DDC’s leverage 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 technology, we are able to design potent oncology-focused chimeric small molecules which combine tumor-targeting specificity with anti-cancer activity of known oncology agents. 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.
