A Randomized, Open-Label Phase 3 Study of Azenosertib Versus Investigator's Choice of Chemotherapy in Platinum-Resistant High-Grade Serous Ovarian, Primary Peritoneal, or Fallopian Tube Cancers Positive for Cyclin E1 Protein Expression

This is a randomized, Phase 3 trial designed to evaluate the efficacy and safety of azenosertib compared to Investigator's choice of chemotherapy in subjects with platinum-resistant ovarian cancer whose tumors are positive for cyclin E1 protein expression.

Start Date17 Apr 2026

Sponsor / Collaborator

K-Group Beta, Inc.

[+1]

NCT06369155

/ RecruitingPhase 2IIT

A Biomarker Study of the Wee1 Inhibitor Azenosertib (ZN-c3) in Women With Recurrent or Persistent Uterine Serous Carcinoma

This research study is being done to investigate how Azenosertib affects tumor cells of persistent or recurrent uterine serous carcinoma.
The name of the study drug involved in this study is:
-Azenosertib (a type of Wee1 inhibitor)

Start Date05 Mar 2025

Sponsor / Collaborator

Dana-Farber Cancer Institute, Inc.

[+2]

NCT06364410

/ RecruitingPhase 1IIT

Phase 1 Study of Trastuzumab Deruxtecan (DS-8201a) in Combination With Azenosertib (ZN-c3) in HER2-Expressing/Amplified Gastric/Gastroesophageal Junction Cancer and Other Solid Tumors

This phase I trial tests the safety, side effects, and best dose of azenosertib in combination with trastuzumab deruxtecan in treating patients with HER2-positive gastric or gastroesophageal junction cancer and other HER2-positive solid tumors that have spread to nearby tissue or lymph nodes (locally advanced), that have spread from where it first started (primary site) to other places in the body (metastatic), or that cannot be removed by surgery (unresectable). Azenosertib is in a class of medications called kinase inhibitors. It inhibits a protein called Wee1. Inhibition of the Wee1 protein can make tumor cells more vulnerable to chemotherapy drugs, leading to tumor cell death. Trastuzumab deruxtecan is in a class of medications called antibody-drug conjugates. It is composed of a monoclonal antibody, called trastuzumab, linked to a chemotherapy drug, called deruxtecan. Trastuzumab attaches to HER2 positive cancer cells in a targeted way and delivers deruxtecan to kill them. Giving azenosertib in combination with trastuzumab deruxtecan may be safe, tolerable, and/or more effective in treating patients with locally advanced, metastatic, or unresectable HER2-positive gastric, gastroesophageal junction, or other solid tumors, compared to just trastuzumab deruxtecan alone.

Start Date03 Feb 2025

Sponsor / Collaborator

National Cancer Institute

100 Clinical Results associated with Azenosertib

100 Translational Medicine associated with Azenosertib

100 Patents (Medical) associated with Azenosertib

Literatures (Medical) associated with Azenosertib

01 Aug 2026·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of APO-50815, a potent WEE1 kinase inhibitor with exceptional efficacy against patient-derived colorectal cancer organoids

Article

Author: Knapp, Stefan ; Barratt, Kate R ; Hasan, Sadia T ; Mukherjee, Siddhartha ; Thomson, Sophie F ; Wright, Josephine A ; Sloan, Erica K ; Priebbenow, Daniel L ; Chang, Aeson ; Baell, Jonathan B ; Kumar, Adarsh ; Woods, Susan L ; Syphers, Joel L ; Worthley, Daniel L ; Leeflang, Julia ; Gee, Yi Sing ; Vrbanac, Laura ; de Nys, Rebekah ; Krämer, Andreas ; Stockton, Kieran ; Silva, Tharindie N ; Young, Savannah ; Lenz, Christopher

Herein, we report the discovery of APO-50815 (14), a potent and selective thietane-3-ol WEE1 inhibitor. When tested against TP53-mutated colorectal cancer (CRC) patient-derived organoids (PDOs) grown from peritoneal and liver metastases, 14 exhibited outstanding anticancer efficacy, surpassing previously reported branched alkane counterpart 3, as well as clinical candidates AZD1775 (1) and ZN-c3 (2). Against primary CRC organoids with diverse TP53, BRAF and KRAS mutation profiles compared with patient-matched normal colon organoids, 14 exhibited selectively potent activity, yielding exceptionally high TI values (129-238) that highlight a substantial therapeutic window for potential cancer treatment. Against primary CRC PDOs (TP53-WT, BRAF-V600E, KRAS-WT), 14 profoundly elevated DNA damage and replication stress compared to 1, while amplifying cellular apoptosis, confirming a broadly similar but superior mode of action. Owing to its highly selective and exemplary anticancer efficacy, 14 represents a valuable tool compound for drug testing investigations against primary and metastatic CRCs, especially in the context of PDOs.

01 Aug 2025·MOLECULAR CANCER THERAPEUTICS

Azenosertib Is a Potent and Selective WEE1 Kinase Inhibitor with Broad Antitumor Activity Across a Range of Solid Tumors

Article

Author: Rutgard, Michael ; Harismendy, Olivier ; Recio-Boiles, Alejandro ; Ma, Jianhui ; Lackner, Mark R. ; Grant, Stephan K. ; Levy, Alexandra ; Li, Jiali ; Cai, Zhen ; Kim, Daehwan ; Liu, Wen ; Bunker, Kevin D. ; Sen, Shiraj ; Doroshow, Deborah B. ; Segar, Jennifer M. ; Fischer, Kimberlee M. ; Samatar, Ahmed A. ; Kim, Sangyub ; Jandial, Danielle

Abstract:

Genomic instability and accumulation of DNA damage are hallmarks of tumor development and progression. To ensure the maintenance of genomic integrity, cells rely on a coordinated DNA damage response network that regulates cell-cycle progression, including activation of WEE1-dependent cell cycle checkpoints. If DNA damage occurs during replication, the WEE1 checkpoint is activated, thereby preventing the progression of the cell cycle. This allows damaged DNA to be repaired before cells enter mitosis, or if the damage is too extensive, induction of apoptosis. These observations have made WEE1 a promising anticancer therapeutic target. Azenosertib (ZN-c3) is a novel, selective, and orally bioavailable WEE1 inhibitor. The antiproliferative activity of azenosertib on cancer cell lines is consistent with a WEE1-dependent mechanism of action exemplified by reduction of pY15-CDK1 levels and increases in DNA damage markers. Azenosertib further exacerbates the effect of replicative stress and DNA damage by allowing cancer cells to prematurely enter mitosis, leading to mitotic catastrophe and apoptosis. Azenosertib has optimized pharmacokinetic and pharmacodynamic properties, yielding robust tumor growth inhibition in a broad range of tumor models, and is highly effective at delaying the duration of tumor regrowth after cessation of treatment. We have explored various dosing schedules in preclinical efficacy models for azenosertib that preserve antitumor activity with minimal toxicity. Phase I studies with azenosertib as monotherapy have shown preliminary clinical activity in patients with advanced solid tumors. The data presented herein support further studies of azenosertib monotherapy across multiple solid tumor indications.

01 Feb 2025·Cancer research communications

The Selective WEE1 Inhibitor Azenosertib Shows Synergistic Antitumor Activity with KRASG12C Inhibitors in Preclinical Models

Article

Author: Lackner, Mark R. ; Harismendy, Olivier ; Kim, Daehwan ; Izadi, Hooman ; Skrable, Blake ; Jameson, Nathan M. ; Guo, Xiao ; Kim, Doris S. ; Ma, Jianhui ; Abed, Mona ; Lee, Catherine ; Shea, Alexandra

Abstract:

Kirsten rat sarcoma (KRAS) is a potent oncogenic driver that results in the downstream hyperactivation of MAPK signaling while simultaneously increasing replication stress (RS) and accumulation of DNA damage. KRASG12C mutations are common and targetable alterations. Therapeutic inhibition of KRASG12C and eventual resistance to these inhibitors are also known to drive RS and DNA damage through adaptive mechanisms that maintain addiction to high MAPK signaling. High levels of RS result in a stronger reliance on cell-cycle checkpoints, thereby introducing a vulnerability to inhibition of cell-cycle checkpoint regulators such as the WEE1 kinase. This provides a rationale for combining azenosertib, a novel, selective, and orally bioavailable WEE1 inhibitor, with KRASG12C inhibitors. An in vitro combination of azenosertib with multiple KRASG12C inhibitors demonstrated synergistic cell growth inhibition across a panel of KRASG12C cell lines in both 2D and 3D assays. In vivo studies demonstrated that azenosertib exhibited significant monotherapy activity as well as synergistic tumor growth inhibition (TGI) when combined with KRASG12C inhibitors, including tumor regression in cell-derived xenograft models of non–small cell lung cancer, colorectal cancer, and pancreatic ductal adenocarcinoma. Importantly, KRASG12C inhibitor–resistant cell-derived xenograft and patient-derived xenograft models demonstrated synergistic TGI in combination arms. Finally, analysis of biomarkers from in vitro and in vivo tumor samples displayed increases in protein markers of RS, DNA damage, and apoptosis after combination treatment. Taken together, our results suggest that the combination of azenosertib with KRASG12C inhibitors enhances TGI over single-agent therapy and may be an effective treatment strategy for patients with KRASG12C tumors.

Significance::

Resistance to KRASG12C inhibitors is a growing clinical concern. The synergistic interaction observed between azenosertib and multiple KRASG12C inhibitors could result in deeper and more durable responses.

132

News (Medical) associated with Azenosertib

29 Jun 2026

·www.biospace.com

4 ovarian cancer candidates to watch: GSK, Allarity and more

iStock, valiantsin suprunovich Recent approvals for Corcept Therapeutics and Merck have injected momentum into the space, where GSK, Allarity Therapeutics, OSE Immunotherapies and others are advancing their own candidates. The market for drugs designed to treat the deadliest gynecological malignancy—ovarian cancer—is gaining steam, thanks to two recent approvals and a crop of novel candidates in earlier-stage trials. In February, Merck secured an FDA approval for Keytruda and subcutaneous injection Keytruda Qlex with paclitaxel for patients with platinum-resistant ovarian cancers (PROC). The addition of the blockbuster immunotherapy led to a 24% reduction in the risk of death, according to Phase 3 trial data. The agency then approved Corcept Therapeutics’ glucocorticoid blocker Lifyorli in PROC in March, with recent data showing a 35% reduction in the risk of death in combination with nab-paclitaxel compared to chemotherapy alone. Both approvals were huge wins, particularly for platinum-resistant ovarian cancer, where treatment options are limited, said Premal Thaker, the WashU Medicine director of gynecological oncology clinical research at Siteman Cancer Center . Thaker is the principal investigator on the Phase 3 OVATION-3 trial, which is evaluating a gene therapy from Imunon called IMNN-001 that is designed to boost levels of IL-12 and change the tumor microenvironment, alongside chemotherapy. Phase 2 data reported in March showed a 14.7-month increase in overall survival compared to standard of care chemotherapy. IMNN-001 is one of several candidates bringing new interest to a stubborn disease with a relative 5-year survival rate of 52% and limited treatment options. “A lot of drugs have gone into trials for many, many decades, and we just haven’t had the same success that we’re seeing right now,” Thaker told BioSpace . “It’s smarter drugs and medications.” Here are four candidates, each with a different mechanism of action, that the field is watching. Make way for GSK’s Mo-Rez and the ADCs The biggest frontrunners poised to make a dent in ovarian cancer are antibody-drug conjugates (ADCs), where AbbVie’s folate receptor antagonist Elahere is first-in-class . Another candidate with recent data is GSK’s mocertatug rezetecan, or Mo-Rez, a novel ADC that targets an antigen called B7-H4 and carries a topoisomerase inhibitor payload. In its Phase 1 dose-escalation trial, BEHOLD-1, Mo-Rez had a confirmed objective response rate (cORR) of 62% in patients with PROC and 67% in those with endometrial cancer, according to data presented at the Society for Gynecological Oncology’s annual meeting in April. “We were pretty happy with that,” Eric Richards, senior vice president and head of medicine development leaders for oncology at GSK, told BioSpace . “What we’re seeing is not only a high level of clinical activity but initial signs of pretty good durability.” Richards added that the immune checkpoint protein B7-H4 is overexpressed in the vast majority of ovarian cancer cells, making it an attractive target. GSK is launching five Phase 3 trials evaluating Mo-Rez this year across ovarian and endometrial cancers, including BEHOLD-Ovarian01 in PROC and BEHOLD-Ovarian02 in platinum-sensitive ovarian cancer. Elsewhere, German biotech Tubulis, recently acquired by Gilead, also recently reported positive results from a Phase 1 trial evaluating its ADC, TUB-040, in PROC. And Daiichi Sankyo and Merck are progressing their candidate raludotatug deruxtecan (R-Dxd) in a Phase 2/3 trial. It’s too early to say which candidates look most promising, Thaker said, adding that many of them carry the same topoisomerase payload. Their side effects will likely be a differentiating factor, she said. “It’s a little bit of a scientific conundrum right now—how are we going to sequence these? Because they all look very exciting.” Cancer ASCO: A battle of bispecifics, Eli Lilly’s big win and more Practice-changing data in lung cancer, prostate cancer and more were on display over the weekend at the American Society of Clinical Oncology annual meeting in Chicago. Plus, early readouts on assets that could reshape the cancer landscape. June 1, 2026 · 4 min read · Brianna Abbott Read more Zentalis chases a new target in WEE1 Zentalis Pharmaceuticals, meanwhile, is enrolling a Phase 3 global trial evaluating its novel inhibitor azenosertib in patients with cyclin E1–positive PROC against standard single-agent chemotherapy, according to a May press release . Azenosertib is designed to inhibit the protein kinase WEE1, a master regulator of cell cycle checkpoints. At the 2026 American Society of Clinical Oncology annual meeting, data from the Phase 1b MUIR trial showed that azenosertib plus paclitaxel resulted in an ORR of 39% and a median progression-free survival (PFS) of 7.3 months in an all-comer PROC population. Both the cyclin E1-positive and negative groups had similar responses, the trial found. The FDA granted Fast Track designation to the drug in January 2025 for patients who are positive for the cyclin E1 protein, which is overexpressed in around half of PROC patients. Ovarian cancer tumors positive for cyclin E1 are often especially hard to treat, Thaker noted. “It’s nice that we’re developing a medication that can help overcome that,” Thaker—who is also involved in the research—said. Plus, she added, the azenosertib pill might be easier to take than some of the ADCs, which are delivered via infusions. OSE’s proof-of-concept for cancer vaccines More positive ovarian cancer data at ASCO 2026 came from OSE Immunotherapeutics, which reported Phase 2 results for its off-the-shelf vaccine Tedopi (OSE2101), designed to stimulate a patient’s T cells and target five different tumor-linked antigens. In the TEDOVA trial, some 185 patients with platinum-sensitive recurrent ovarian cancer (PSOC) were randomized to Tedopi, Tedopi plus pembrolizumab or best supportive care as maintenance treatment after chemo. Patients in the trial were also required to be HLA-A2 positive, which shrinks the number of potentially eligible patients, Thaker said. “We have to be mindful when we look at some of these targets, we have to cut the pie a little bit more.” With a median follow-up of 22 months, patients on Tedopi and pembrolizumab experienced a median PFS of 4.1 months, compared to 2.8 months for those getting the best supportive care. The addition of pembrolizumab to Tedopi led to a 28% reduction in the risk of progression or death, compared to Tedopi alone, the trial found, though that result missed the mark for statistical significance. The results are the first proof of concept for a therapeutic vaccine in ovarian cancer and the first positive trial for PSOC in years, Alexandra Leary, deputy head of the department of medical oncology at Gustave Roussy in France and lead investigator on the trial, said in a press release . Allarity’s next generation PARP inhibitor Allarity Therapeutics’ stenoparib is another candidate with FDA Fast Track designation. The drug is a dual-target inhibitor that homes in on PARP 1/2 and tankyrase 1/2, differentiating it from earlier PARP inhibitors such as AstraZeneca and Merck’s Lynparza and GSK’s Zejula. Inhibiting tankyrase can disrupt signaling in the WNT pathway, which has been implicated in multiple cancers, Jeremy R. Graff, president and chief developmental officer at Allarity, told BioSpace . “It really seems to be particularly highly activated in really advanced, chemo- and radio-resistant cancers.” Allarity licensed stenoparib in 2017 from Eisai based on the drug’s Phase 1 data. In Phase 2 data reported in September 2025, the median overall survival had not been reached at 25 months for patients with platinum-resistant and refractory ovarian cancer. The drug appeared to benefit patients regardless of their BRCA status, Graff added. The company is expanding its Phase 2 trial for patients with PROC and has amended its trial protocol to focus on advanced, recurrent, platinum-resistant or platinum-ineligible ovarian cancer. Like with Zentalis’s azenosertib, the pill will likely be easier to take with milder toxicities than the ADCs, Graff said, which could be particularly helpful for older women. Ovarian cancer hasn’t historically garnered as much attention as cancers with the biggest patient pools, including breast or prostate cancer, Graff said. But the hard-to-treat disease is now capturing more interest. “It’s a huge unmet medical need,” Graff said. “We’d love to, with the era of targeted therapies, go beyond just poisoning people with chemotherapy.” .responsive-container { display: flex; flex-wrap: wrap; border: 1px solid #ededed; font-family: Helvetica, Arial, Sans-Serif; padding: 20px 20px 10px 20px; } .column-left { flex: 1; max-width: 45%; padding: 20px 20px 10px 20px; } .column-right { flex: 2; padding: 20px 20px 10px 20px; } @media (max-width: 768px) { .column-left, .column-right { max-width: 100%; flex: 100%; padding: 10px 0; } } Subscribe to ClinicaSpace! Clinical trial results, research news, the latest in cancer, cell and gene therapy hbspt.forms.create({ region: "na1", portalId: "4413123", formId: "674f4dc0-7371-4190-86cc-e1afd00b08ea", onFormSubmitted: function($form, data) { window.dataLayer = window.dataLayer || []; window.dataLayer.push({ 'event': 'GTMevent', 'event_name': 'newsletter_sign_up' }); } });

Clinical ResultPhase 3Phase 1ASCOPhase 2

02 Jun 2026

·www.biospace.com

Zentalis Pharmaceuticals Announces Inducement Grants Under Nasdaq Listing Rule 5635(c)(4) - June 1, 2026

SAN DIEGO, June 01, 2026 (GLOBE NEWSWIRE) -- Zentalis ® Pharmaceuticals, Inc. (Nasdaq: ZNTL), a clinical oncology innovator advancing late-stage development of investigational first-in-class WEE1 inhibitor azenosertib as a biomarker-driven treatment approach for ovarian cancer, today announced that on June 1, 2026, the Compensation Committee of Zentalis’ Board of Directors granted non-qualified stock options to purchase an aggregate of 191,000 shares of the Company’s common stock to two (2) newly hired employees. The stock options were granted under the Zentalis Pharmaceuticals, Inc. 2022 Employment Inducement Incentive Award Plan (2022 Inducement Plan) as an inducement material to each such individual’s entering into employment with Zentalis in accordance with Nasdaq Listing Rule 5635(c)(4). The 2022 Inducement Plan is used exclusively for the grant of equity awards to individuals who were not previously employees of Zentalis, or following a bona fide period of non-employment, as an inducement material to each such individual’s entering into employment with Zentalis, pursuant to Nasdaq Listing Rule 5635(c)(4). The stock options have an exercise price of $3.98 per share, which is equal to the closing price of Zentalis’ common stock on The Nasdaq Global Market on the date of grant. The stock options have a 10-year term and will vest over four years, with 25% of the options vesting on the first anniversary of the vesting commencement date and the remaining 75% of the options vesting in equal monthly installments over the three years thereafter. Vesting of the stock options is subject to the employee’s continued service to Zentalis on each vesting date. About Zentalis Pharmaceuticals Zentalis is a clinical oncology innovator developing a treatment approach for ovarian cancer and multiple tumor types. Leveraging therapeutics development and biomarker expertise, Zentalis is advancing monotherapy and combination studies of its investigational first-in-class WEE1 inhibitor, azenosertib. Focused on translating WEE1 science into clinical practice, we aim to equip physicians with a targeted, non-chemo, orally available medicine that enhances treatment experience, choice, and outcomes. Our mission: to unburden cancer patients with more convenience and care. For more information, please visit . Follow Zentalis on LinkedIn at . ZENTALIS ® and its associated logo are trademarks of Zentalis and/or its affiliates. All website addresses and other links in this press release are for information only and are not intended to be an active link or to incorporate any website or other information into this press release. Contact: Aron Feingold VP, Investor Relations & Corporate Communications ir@zentalis.com

27 May 2026

·www.biospace.com

Zentalis Strengthens Commercial Leadership with Appointments of Shannon Campbell to Board of Directors and Sarah Kelly as SVP of Commercial Strategy

Appointments enhance commercialization readiness as Zentalis advances registrational program for azenosertib in Cyclin-E1 positive platinum-resistant ovarian cancer SAN DIEGO, May 27, 2026 (GLOBE NEWSWIRE) -- Zentalis® Pharmaceuticals, Inc. (Nasdaq: ZNTL), a clinical oncology innovator advancing late-stage development of investigational first-in-class WEE1 inhibitor azenosertib as a biomarker-driven treatment approach for ovarian cancer, today announced the appointments of Shannon Campbell to its Board of Directors and Sarah Kelly as the Company’s Senior Vice President of Commercial Strategy. These appointments reflect Zentalis’ continued commitment to developing commercial and operational capabilities as the Company advances registration-intended Phase 2 and Phase 3 trials of azenosertib for patients with Cyclin E1-positive platinum-resistant ovarian cancer (PROC). “Shannon Campbell brings deep experience helping oncology companies successfully navigate the transition from clinical to commercial-stage,” said Julie Eastland, Chief Executive Officer of Zentalis. “Shannon’s commercial scale-up leadership will help us achieve our vision as we continue advancing azenosertib through late-stage development for patients with Cyclin E1-positive platinum-resistant ovarian cancer (PROC). Simultaneously, the appointment of Sarah Kelly brings a broad set of experience in building launch readiness for both companion diagnostics and therapeutics. Together, these roles provide the strategic, operational, and commercial foundation needed to support launch readiness and long-term growth.” Ms. Campbell is a seasoned biopharmaceutical executive with more than 30 years of experience, leading global commercial strategy and building oncology franchises. Her proven track record will support Zentalis as it advances toward the potential commercialization of azenosertib for Cyclin E1 positive PROC patients, as well as, evaluating azenosertib in earlier lines of ovarian cancer, as a combination therapy, and in other tumor types. Most recently, Ms. Campbell served as Executive Vice President and Chief Commercial Officer at Merus, where she led the company’s evolution toward becoming a commercial-stage organization, including launch preparedness efforts for its portfolio of multiclonic antibodies. Prior to Merus, she held senior oncology leadership roles at Novartis Pharmaceuticals and Bayer Healthcare Pharmaceuticals, where she supported the launch and growth of innovative therapies across solid tumors and rare diseases. Ms. Campbell currently serves on the board of Black Diamond Therapeutics and is an advisory board member for Verix. “I am excited to join Zentalis’ Board at an important time for the Company as it prepares to bring a potential first-in-class therapy to market for patients with platinum-resistant ovarian cancer, a population with significant unmet need,” said Ms. Campbell. “I look forward to working with the Zentalis Board and the leadership team to help build the strategic and commercial infrastructure needed to ultimately bring this important potential new treatment option to the community.” Sarah Kelly joins Zentalis as Senior Vice President of Commercial Strategy to lead launch readiness. Throughout Ms. Kelly’s 30-year career, she has held senior leadership positions in commercial and business development at companies including Amgen, Turning Point, Spectrum and Agilent. Ms. Kelly’s extensive experience in oncology includes building and leading commercial organizations in preparation for therapeutic and companion diagnostic launches. Ms. Kelly’s focus on commercial strategy, market access, companion diagnostics, field leadership, and business development provides operational expertise to prepare Zentalis for the potential to bring azenosertib to patients. Zentalis is advancing azenosertib through a late-stage registrational development program in Cyclin E1-positive PROC, with an anticipated year-end 2026 topline readout from the DENALI Phase 2 trial, which is designed to support a potential accelerated approval pathway, pending data outcomes and U.S. FDA feedback. Additionally, Zentalis recently announced dosing of the first patient in the ASPENOVA Phase 3 confirmatory trial in Cyclin E1-positive PROC, which is designed to support conversion from accelerated to full approval, as well as potential ex-U.S. registrations. About Azenosertib Azenosertib is an investigational, potentially first-in-class, selective, and orally bioavailable inhibitor of WEE1 currently being evaluated in clinical studies in ovarian cancer and additional tumor types. WEE1 acts as a master regulator of the G1-S and G2-M cell cycle checkpoints, through negative regulation of both CDK1 and CDK2, to prevent replication of cells with damaged DNA. By inhibiting WEE1, azenosertib enables cell cycle progression, despite high levels of DNA damage, thereby resulting in the accumulation of DNA damage and leading to mitotic catastrophe and cancer cell death. Azenosertib is in late-stage development as a potential treatment for Cyclin E1-positive platinum-resistant ovarian cancer (PROC). There is currently no approved treatment option specifically for this biomarker-selected population which comprises approximately 50% of PROC patients. Cyclin E1 protein overexpression has been established as a sensitive and specific predictive biomarker for identifying patients who could potentially derive benefit from azenosertib treatment, based on retrospective analysis of azenosertib studies in PROC. Validation of the Cyclin E1 companion diagnostic assay is ongoing in the DENALI and ASPENOVA trials. Azenosertib has been granted Fast Track Designation by the U.S. FDA for the treatment of patients with Cyclin E1-positive platinum-resistant ovarian cancer. Fast Track Designation is intended to facilitate the development and expedite the review of therapies that have the potential to treat serious conditions and address unmet medical needs. About Zentalis Pharmaceuticals Zentalis is a clinical oncology innovator developing a treatment approach for ovarian cancer and multiple tumor types. Leveraging therapeutics development and biomarker expertise, Zentalis is advancing monotherapy and combination studies of its investigational first-in-class WEE1 inhibitor, azenosertib. Focused on translating WEE1 science into clinical practice, we aim to equip physicians with a targeted, non-chemo, orally available medicine that enhances treatment experience, choice, and outcomes. Our mission: to unburden cancer patients with more convenience and care. For more information, please visit . Follow Zentalis on LinkedIn at . Forward-Looking Statements This press release contains forward-looking statements within the meaning of the U.S. Private Securities Litigation Reform Act of 1995, as amended. All statements contained in this press release that do not relate to matters of historical fact should be considered forward-looking statements, including, but not limited to, statements regarding the continued development of azenosertib; the clinical and therapeutic potential of azenosertib as a monotherapy and as a combination agent; the potential for azenosertib to be first-in-class; the potential benefits of azenosertib across multiple lines of ovarian cancer and other tumor types; the combinability of azenosertib with other agents and the potential benefits thereof; the broad franchise potential of azenosertib; the Company’s biomarker-driven strategy for azenosertib; the potential regulatory approval and commercialization of azenosertib; the Company’s anticipated milestones and the timing thereof, including the anticipated timing of the topline readout from DENALI Part 2; the Company’s launch readiness and long-term growth; and the building of the Company’s the strategic and commercial infrastructure. The terms “achieve,” “anticipate,” “advance,” “build,” “design,” “develop,” “expect,” “focus,” “growth,” “look forward,” “potential,” “strategy,” “strengthen,” “support,” “target,” and “will” and similar references are intended to identify forward-looking statements, although not all forward-looking statements contain these identifying words. These statements are neither promises nor guarantees, but involve known and unknown risks, uncertainties and other important factors that may cause our actual results, performance or achievements to be materially different from any future results, performance or achievements expressed or implied by the forward-looking statements, including, but not limited to, the following: our limited operating history, which may make it difficult to evaluate our current business and predict our future success and viability; we have and expect to continue to incur significant losses; our need for additional funding, which may not be available; our substantial dependence on the success of azenosertib; our plans, including the costs thereof, of development of companion diagnostics; the outcome of preclinical testing and early trials may not be predictive of the success of later clinical trials; potential unforeseen events during clinical trials could cause delays or other adverse consequences; risks relating to the regulatory approval process or ongoing regulatory obligations; our product candidates may cause serious adverse side effects; the interim, initial, “topline,” and preliminary data from our clinical trials may change as more patient data becomes available, and are subject to audit and verification procedures that could result in material changes in the final data; our reliance on third parties; effects of significant competition; the possibility of system failures or security breaches; risks relating to intellectual property; our ability to attract, retain and motivate qualified personnel, and risks relating to management transitions; significant costs as a result of operating as a public company; and the other important factors discussed under the caption “Risk Factors” in our most recently filed periodic report on Form 10-K or 10-Q and subsequent filings with the U.S. Securities and Exchange Commission (SEC) and our other filings with the SEC. Any such forward-looking statements represent management’s estimates as of the date of this press release. While we may elect to update such forward-looking statements at some point in the future, we disclaim any obligation to do so, even if subsequent events cause our views to change. ZENTALIS ® and its associated logo are trademarks of Zentalis and/or its affiliates. All website addresses and other links in this press release are for information only and are not intended to be an active link or to incorporate any website or other information into this press release. Contact: Aron Feingold VP, Investor Relations & Corporate Communications ir@zentalis.com

100 Deals associated with Azenosertib

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	United States	K-Group Beta, Inc.	17 Apr 2026
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Australia	K-Group Beta, Inc.	17 Apr 2026
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Belgium	K-Group Beta, Inc.	17 Apr 2026
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Canada	K-Group Beta, Inc.	17 Apr 2026
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	France	K-Group Beta, Inc.	17 Apr 2026
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Germany	K-Group Beta, Inc.	17 Apr 2026
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Ireland	K-Group Beta, Inc.	17 Apr 2026
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Italy	K-Group Beta, Inc.	17 Apr 2026
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	Poland	K-Group Beta, Inc.	17 Apr 2026
Platinum-Resistant Fallopian Tube Carcinoma	Phase 3	South Korea	K-Group Beta, Inc.	17 Apr 2026

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04516447 (Zn-c3-002, ESGO2026)	Phase 1	Ovarian Cancer Maintenance Cyclin E1 positive	14	Azenosertib plus bevacizumab	rhobpfbfcp(qpjragjzsn) = The majority of treatment-related adverse events were grade 1-2, with the most common being paronychia (57.1%, all grade 1) and owwctqdaur (sggbowcneu ) View more	Positive	28 Feb 2026
NCT05743036 (Phase 1 dose escalation results of the WEE1 inhibitor, ASCO2025)	Phase 1	Metastatic Colorectal Carcinoma BRAF V600E	44	Azenosertib	jixpsceqhm(ejqbgcmatj) = 11.4% hewnyhxxta (ahojhkokom ) View more	Positive	30 May 2025
NCT05198804 \| NCT05128825 \| NCT04158336 (AACR2025)	Not Applicable	Ovarian Serous Tumor TP53 mutations	139	Azenosertib 300mg QD	thsbkhympk(elkfylyntv) = thoxmbdsvb rnaxhisolw (pfzzeleizx ) View more	Positive	28 Apr 2025
NCT05198804 \| NCT05128825 \| NCT04158336 (AACR2025)	Not Applicable	Ovarian Serous Tumor TP53 mutations	139	Placebo	thsbkhympk(elkfylyntv) = idrtwuozmj rnaxhisolw (pfzzeleizx ) View more	Positive	28 Apr 2025
NCT05128825 (DENALI, Company_Website) Manual	Phase 2	Platinum-Resistant Ovarian Carcinoma CCNE1 Amplification	102	Azenosertib 400mg QD 5:2 dose	aufbddyvga(yqyzpcixlu) = zxftyurnax ezkevgncoi (dvvktmemla, 21.0 - 50.9) View more	Positive	15 Mar 2025
NCT04833582 (ASCO2024)	Phase 1	Osteosarcoma, Recurrent	31	Azenosertib	pykkzruuai(bkqblvgmug) = skthdjfpwi jvowqqqdbi (xqhfruiijp )	Positive	24 May 2024
NCT04516447 (ASCO 12023 \| ASCO 22023) Manual	Phase 1	Primary peritoneal carcinoma \| Ovarian Epithelial Carcinoma \| Fallopian Tube Carcinoma	94	Paclitaxel+Azenosertib	mvoscwzzmq(humjpbmtqv) = neutropenia (44.4), thrombocytopenia (30.3), anemia (12.1), leukopenia (11.1), fatigue (10.1), diarrhea (6.1), nausea (5.1), and vomiting (5.1) kbsfpbxqxg (qqziffyzux )	Positive	26 May 2023
NCT04516447 (ASCO 12023 \| ASCO 22023) Manual	Phase 1		94	Carboplatin+Azenosertib		Positive	26 May 2023
NCT04516447 (AACR2022) Manual	Phase 1	Ovarian Cancer \| Primary peritoneal carcinoma \| Fallopian Tube Carcinoma Second line \| Third line	41	total	bcpmkvsbia(ebypjlydxs) = nausea 7.3%, neutropenia 34.1%, thrombocytopenia 17.1%, anemia 9.8%, diarrhea 2.4%, fatigue 2.4%, vomiting 9.8%, leukopenia 7.3%, abdominal pain 7.3%, hypoalbuminemia 2.4%, alanine aminotransferase increased 7.3%, and hypomagnesemia 2.4% ugmlgiuwcj (okfiawdwgr ) View more	Positive	15 Jun 2022
NCT04516447 (AACR2022) Manual	Phase 1		41	carboplatin+ZN-c3		Positive	15 Jun 2022
NCT04158336 (ZN-c3-001, AACR2022) Manual	Phase 1	Uterine Serous Carcinoma	12	ZN-c3	fqcsvykmvk(qvodqnncvo) = jcrexthoaj nllgrdaxin (idbqlarfrs ) View more	Positive	15 Jun 2022
NCT04158336 (ZN-c3-001, AACR 12021 \| AACR 22021) Manual	Phase 1	HR-positive/HER2-low Solid Tumors	39	ZN-c3	kdssioicsf(svcbnigrto) = tnwofuuojt prgnhcfjkm (bjotfcrbki ) View more	Positive	10 Apr 2021

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