Zentalis Pharmaceuticals is a clinical-stage biopharmaceutical company dedicated to advancing cancer treatment through the development of small molecule therapeutics. Their primary focus is on targeting fundamental biological pathways associated with various cancers, utilizing a deliberate approach to medicinal chemistry. One of their key product candidates, Azenosertib, is a first-in-class WEE1 inhibitor designed to induce cancer cell death by preventing the repair of damaged DNA, thereby pushing these cells into mitosis. This innovative therapeutic is being evaluated across multiple clinical trials for various indications, including gynecologic malignancies and other solid tumors, highlighting its potential to address significant unmet medical needs in oncology.

The company employs an Integrated Discovery Engine, which streamlines the process of identifying and developing novel oncology therapies. This approach encompasses a thorough assessment of cancer biology, the evaluation of chemical scaffolds, and the creation of new molecules aimed at overcoming the limitations of existing treatments. By leveraging their extensive expertise in medicinal chemistry and cancer biology, Zentalis has successfully advanced multiple candidates through the FDA's Investigational New Drug (IND) process, demonstrating their commitment to improving patient outcomes through innovative cancer therapies.

United States

We are dedicated to the discovery and development of small molecule therapeutics targeting fundamental biological pathways of cancer. Our experienced team is comprised of industry leaders with proven track records in the discovery, clinical development, and commercialization of innovative cancer therapies. Leveraging our extensive industry experience and know-how, we developed our Integrated Discovery Engine—our working model for generating potentially differentiated product candidates that are designed to target distinct cancer pathways. This approach has allowed us to advance a diverse pipeline in a capital efficient manner, clearing four INDs with the FDA in five years. We believe our deep pipeline of oncology therapeutic candidates has the potential to significantly improve the lives of patients with various types of cancer.

In May 2020, we established Zentera Therapeutics, our majority-owned Chinese joint venture, to develop and commercialize three Zentalis-discovered oncology candidates (ZN-c5, ZN-c3, and ZN-d5), in addition to potential future candidates, in China. The launch of Zentera is a key milestone in our global clinical development strategy and is the first step toward advancing our potentially best-in-class therapeutic candidates to markets worldwide.

Cancer

Zentalis Pharmaceuticals

Uterine disease

ZN-c3 is an oral inhibitor of WEE1 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. We believe ZN-c3 has broad potential to treat patients with cancer, both as a monotherapy and in combination, including with chemotherapy agents, PARP inhibitors and other targeted therapies.

Azenosertib (ZN-c3) (oral inhibitor of WEE1)

Ovarian cancer

Platinum-resistant ovarian cancer

ZN-c3 is an oral inhibitor of WEE1 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. Zentalis is currently conducting a Phase 1/2 clinical trial of ZN-c3 as a monotherapy in patients with advanced solid tumors, and a Phase 1b clinical trial evaluating ZN-c3 in combination with chemotherapy in patients with advanced ovarian cancer.

Azenosertib (ZN-c3) (oral inhibitor of WEE1) mono

PARPi Resistant Ovarian Cancer

Azenosertib (ZN-c3) (oral inhibitor of WEE1) +/- niraparib

Azenosertib (ZN-c3) (oral inhibitor of WEE1) w/ multiple chemo

Solid tumor/s

Azenosertib (ZN-c3) (oral inhibitor of WEE1) 

Platinum Sensitive Ovarian Cancer

Osteosarcoma

Azenosertib (ZN-c3) + gemcitabine

Breast cancer

Our lead product candidate, ZN-c5, is an 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-c5: Oral SERD (Monotherapy)

ZN-c5 (Oral SERD) +Verzenio® (abemaciclib)

Acute myeloid leukemia

ZN-d5 is an oral inhibitor of B-cell lymphoma 2 (BCL-2), in development initially for the treatment of hematologic malignancies. BCL-2 plays a critical role in the regulation of cell death and the overexpression of this protein is frequently detected in numerous cancer types, preventing apoptosis. Zentalis believes a BCL-2 inhibitor will restore the normal apoptosis process. The Company has initiated a Phase 1 trial of ZN-d5 in patients with AML and Non-Hodgkin's Lymphoma.

Zentalis Pharmaceuticals

Company Details