Our Pipeline

Pipeline

Candidate NameCand
PreclinicalPre
Phase 1Ph 1
Phase 2Ph 2
Phase 3Ph 3
CollaboratorsCollab
ZN-c3: Wee1 Inhibitor
Pfizer - GSK - Zentera logos
Pfizer - GSK - Zentera logos
Monotherapy

ZN-c3: Wee1 Inhibitor

Uterine Serous Carcinoma*
Uterine Serous Carcinoma+USC+
Biomarker-Driven*
Biomarker-Driven*Biomarker*
Solid Tumors
Solid TumorsSolid Tumors
Combination

ZN-c3: Wee1 Inhibitor

Osteosarcoma (+ gemcitabine)*
Osteosarcoma (+ gemcitabine)*Osteosarcoma
Ovarian Cancer (+ niraparib)
Ovarian Cancer (+ niraparib)Ov Cancer
Ovarian Cancer (+ chemo)
Ovarian Cancer (+ chemo)Ov Cancer
ZN-d5: BCL-2 Inhibitor
Zentera logo
Zentera logo
Monotherapy

ZN-d5: BCL-2 Inhibitor

AL Amyloidosis*
AL Amyloidosis*AL Amyloidosis*
AML + Non-Hodgkin’s Lymphoma
AML + Non-Hodgkin’s LymphomaAML + Non-Hodgkin’s Lymphoma
Combination

ZN-d5: BCL-2 Inhibitor

AML (+ ZN-c3)AML (+ ZN-c3)
ZN-c5: Oral SERD
Zentera logo
Zentera logo
Monotherapy

ZN-c5: Oral SERD

Breast Cancer
Breast CancerBrst Cancer
ZN-e4: EGFR Inhibitor
SciClone logo
SciClone logo
Monotherapy

ZN-e4: EGFR Inhibitor

NSCLC
NSCLCNSCLC
BCL-xL Degrader
Monotherapy

BCL-xL Degrader

Solid Tumors and Hematology MalignanciesSolid Tumors and Heme Malignancies

+ Registrational trial with FDA Fast Track designation
* Potentially registrational trial

Product Candidates

Our lead product candidate, ZN-c3, is a potentially first-in-class and best-in-class oral Wee1 inhibitor in development for the treatment of advanced solid tumors. The inhibition of Wee1, a DNA damage response protein, aims to generate sufficient DNA damage in cancer cells, causing cell death, thereby preventing tumor growth and potentially causing tumor regression. Currently, there are no FDA-approved Wee1 inhibitors, and we have designed ZN-c3 to have advantages over other investigational therapies with superior solubility, selectivity, and PK properties. 

ZN-c3 has broad potential as a monotherapy and in combination and we are currently evaluating this candidate in several ongoing and planned studies, including two potentially registrational monotherapy trials in USC and a biomarker-driven setting, as well as combination studies with chemotherapy and GSK’s niraparib (Zejula®) in patients with advanced ovarian cancer. We also recently received orphan drug and rare pediatric disease designations by the FDA for osteosarcoma and initiated a Phase 1/2 trial in combination with chemotherapy. Additionally, we will support two planned investigator-initiated trials with the Ivy Brain Center in glioblastoma multiforme (GBM) and with Dana Farber in combination with immunotherapy in triple negative breast cancer.

ZN-d5 is our oral selective inhibitor of B-cell lymphoma 2 (BCL-2), in development initially for the treatment of hematologic malignancies and related disorders. BCL-2 and BCL-xL are proteins that play a critical role in the regulation of cell death. The overexpression of BCL-2 and/or BCL-xL are frequently detected in numerous cancer types, which prevent apoptosis of cancer cells. We believe a BCL-2 inhibitor will restore the normal apoptosis process, making it an important target for cancer treatments. Utilizing our medicinal chemistry expertise, we have designed ZN-d5 to have optimized potency, selectivity and PK. 

We believe ZN-d5 is an attractive candidate for evaluation as a monotherapy and in combination with other therapies and we are currently conducting a Phase 1 trial of ZN-d5 in patients with AML and Non-Hodgkin’s lymphoma (NHL) and a potentially registrational Phase 1/2 trial in patients with relapsed or refractory Light Chain (AL) amyloidosis. Future clinical development will also include combination studies. 

ZN-c5 is a potentially best-in-class oral selective estrogen receptor degrader (SERD) being developed for the treatment of ER+/HER2- advanced or metastatic breast cancer. ER+/HER2- breast cancer, which is reliant on the estrogen receptor (ER) for tumor growth and survival, affects approximately 70% of all breast cancer patients in the U.S. and is currently treated using a number of approved hormonal therapies. Despite treatment advances, we believe the currently approved hormonal therapies—including the only FDA-approved SERD— have limitations that create an opportunity for the development of a differentiated candidate. We have designed ZN-c5 to overcome these limitations and have a potentially superior product profile with convenient oral administration.

ZN-e4 is our oral, small molecule inhibitor of mutant epidermal growth factor receptor (EGFR) initially being developed for the treatment of non-small-cell lung carcinoma (NSCLC). EGFR regulates many cellular functions, including cell proliferation and survival, and is responsible for tumor growth in a number of cancers, including lung cancer. The inhibition of EGFR has already been clinically validated as an effective approach to treating NSCLC. However, the FDA-approved third-generation inhibitor of EGFR still has toxicities, including skin rashes, associated with first- and second-generation inhibitors. ZN-e4 is designed to achieve a similar potency and inhibition of EGFR, but is also designed to be more selective, tolerable and soluble in comparison to the current approved therapies.

Our Phase 1/2 trial of ZN-e4 in patients with advanced NSCLC with activating EGFR mutations is ongoing and continues to enroll. We are also actively evaluating potential combination therapies for the future clinical development of ZN-e4.