On May 21, 2026 Merck, a leading science and technology company, reported that the first patient has been dosed in the Phase 3 PROCEADE-CRC-03 trial (NCT07549412). The study is evaluating precemtabart tocentecan (Precem‑TcT), a potential first‑in‑class investigational anti‑CEACAM5 antibody‑drug conjugate (ADC), for the treatment of metastatic colorectal cancer (mCRC).

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"Leveraging our novel payload‑linker technology, Precem‑TcT is the first CEACAM5‑targeted ADC in clinical studies with an exatecan payload, rationally designed for stability and enhanced cancer cell killing activity," said David Weinreich, MD, MBA, Global Head of R&D and Chief Medical Officer for the Healthcare business of Merck. "The Phase 3 study and the enrollment of the first patient with Precem-TcT build on the Company’s more than 20 years of expertise in colorectal cancer, and highlight our commitment to advancing differentiated ADCs for heavily pretreated patients with limited treatment options."

The PROCEADE-CRC-03 study assesses the efficacy and safety of Precem-TcT, alone or with bevacizumab, in patients with mCRC who are intolerant- or refractory-to, or progressed after, systemic therapies. The PROCEADE-CRC-03 study will be conducted in approximately 165 sites in 20 countries and will recruit approximately 1,020 patients with mCRC.

In Phase 1 (PROCEADE-CRC-01; NCT05464030), Precem-TcT as monotherapy or in combination showed predictable and manageable safety in more than 100 patients with heavily pretreated mCRC. At the recommended dose for Phase 3 development (2.8 mg/kg Q3W; n=29), confirmed objective response rate (cORR) was 20.7% (95% CI: 8.0, 39.7), median PFS was 6.9 months (95% CI: 4.4, 9.5) and median OS was not reached (95% CI: 8.7, NE) after a median follow-up of 13.1 months.

"The PROCEADE-CRC-03 Phase 3 study is designed to address significant unmet needs for patients with metastatic colon cancer whose disease has progressed after standard therapies," said Kanwal P.S. Raghav, MBSS, MD, Department of Gastrointestinal Medical Oncology, MD Anderson Cancer Center, Houston. "The data from the phase 1 study suggested a manageable safety profile for Precem-TcT and encouraging early tumor response in the patients with heavily pre-treated metastatic colorectal cancer. CEACAM5 is largely absent from healthy tissues and is overexpressed in nearly all mCRC cases, supporting a non-selective, universal patient approach, and represents a promising therapeutic target in this setting."

Globally, CRC is the third-most commonly diagnosed malignancy and the second leading cause of cancer-related deaths.1 Merck chose mCRC as the first indication to assess the efficacy and safety of Precem-TcT because ~90% of colorectal cancers overexpress CEACAM5,2 and there is a high unmet clinical need in patients with metastatic colorectal cancer, especially among those who progressed on several previous therapies.3,4,5 Patients with advanced colorectal cancer typically face a challenging prognosis, with few options available for those whose disease continues to progress after three or more lines of therapy. Additionally, with progression, response to treatment and prognosis become increasingly worse over time.

Advancing the Future of Cancer Care

At Merck, we strive every day to improve the futures of people living with cancer. Building on our 350-year global heritage as pharma pioneers, we are focusing our most promising science to target cancer’s deepest vulnerabilities, pursuing differentiated molecules to strike cancer at its core. By developing new therapies that can help advance cancer care, we are determined to create a world where more cancer patients will become cancer survivors. Learn more at www.merckgroup.com.

About Precemtabart tocentecan (M9140)

Precemtabart tocentecan is an investigational anti-CEACAM5 antibody-drug conjugate (ADC). Leveraging the company’s novel linker-payload technology, precemtabart tocentecan is the first CEACAM5 ADC with an exatecan payload, a potent topoisomerase inhibitor (TOP1i), which has been rationally designed for stability in circulation and superior cancer cell killing activity. Beyond the direct effect on the target cell, precemtabart tocentecan has been shown in preclinical research to induce tumor cell death through a bystander effect in which exatecan permeates the cell membrane to neighboring cells, inducing apoptosis (cell death). This bystander effect within the tumor microenvironment may enhance efficacy. Precemtabart tocentecan is currently being evaluated across tumor types with CEACAM5 expression and a high unmet need, including metastatic colorectal cancer (mCRC), gastric cancer (GC), non-small cell lung cancer (NSCLC), and pancreatic ductal adenocarcinoma (PDAC).

About Colorectal Cancer

Colorectal cancer (CRC) is cancer of the colon or rectum, which often arises from benign polyps that eventually turn cancerous. It is the third most common diagnosed malignancy, and the second leading cause of cancer deaths worldwide with approximately 1 in 10 cancer deaths attributed to CRC. Despite new therapies, 5-year survival of stage 4 CRC is <20%. The global burden of CRC has substantially increased over time and is expected to increase by 60% to more than 2.2 million new cases and 1.1 million deaths by 2030.

(Press release, Merck & Co, MAY 21, 2026, View Source [SID1234665977])

On May 21, 2026 BlossomHill Therapeutics, Inc., a privately-held, clinical-stage biopharmaceutical company applying an intentional, chemistry-based approach to design and develop innovative small molecule medicines for the treatment of cancer, reported an upcoming presentation of the preliminary, Phase 1 dose escalation/backfill data from the company’s ongoing Phase 1/2 SOLARA clinical trial of BH-30643 in epidermal growth factor receptor (EGFR)-mutant non-small cell lung cancer (NSCLC). The data will be presented in an oral session at the 2026 American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting on Tuesday, June 2, 2026.

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BH-30643 is a non-covalent, macrocyclic, brain active, mutant-selective OMNI-EGFR inhibitor designed to address a broad spectrum of EGFR mutations, including classical mutations, on-target resistance mutations such as C797S (with or without T790M), atypical mutations and exon 20 insertion mutations.

"BH-30643 represents a potentially important advancement in the evolution of targeted therapies for treating EGFR mutant NSCLC," said Xiuning Le, M.D., Ph.D., Associate Professor in Medical Oncology at the MD Anderson Cancer Center. "Using a novel macrocyclic approach, BH-30643 has the potential to impact multiple clinically relevant EGFR mutation classes while minimizing inhibition of wild-type EGFR. The response data we are presenting at ASCO (Free ASCO Whitepaper) are encouraging – in a heavily pretreated Phase 1 dose escalation/backfill population, in patients with brain metastases, and even in the difficult-to-treat C797S/T790M population. These findings suggest BH-30643’s potential to address a significant unmet need for patients, especially those whose disease has progressed on prior EGFR TKIs."

"These Phase 1 dose escalation/backfill data demonstrated encouraging clinical activity for BH-30643, with a favorable tolerability profile in the setting of high PK exposures, and with responses observed across a broad range of EGFR genotypes," said Geoff Oxnard, M.D., Chief Medical Officer of BlossomHill Therapeutics. "Importantly, we are seeing confirmed responses in patients harboring C797S resistance mutations, a population where current treatment options remain limited and outcomes are poor. We believe these findings support the potential for BH-30643 to address significant unmet need. Phase 1 dose expansion is ongoing to determine the recommended Phase 2 dose and support further clinical development, with an initial focus on patients with C797S-positive resistance."

Key presentation highlights to include:

Preliminary results (March 2, 2026, data cut, with efficacy follow-up through April 29, 2026) from the Phase 1 dose escalation/backfill in Phase 1/2 SOLARA trial in patients with heavily pretreated and heterogeneous EGFR-mutant NSCLC. The Phase 1 dose escalation/backfill portion enrolled 82 patients (median of 3 prior lines of therapy, 66% with history of brain metastases, and 71% ECOG=1) across dose cohorts ranging from 20 mg to 160 mg total daily dose of BH-30643.
High plasma exposures were observed that exceeded target EC90 at candidate doses.
BH-30643 demonstrated a favorable tolerability profile with primarily low-grade EGFR wildtype toxicity as well as asymptomatic Gilbert’s-like bilirubin elevation; Grade ≥2 EGFR-wildtype treatment related adverse events (TRAEs) were reported in 27% of patients. No clinically significant cardiac effects were seen.
Responses and prolonged stable disease were observed across diverse EGFR genotypes in a heavily pretreated Phase 1 cohort, suggesting effective targeting of on-target resistance.
32 patients with C797S mutations were response evaluable across escalation and expansion cohorts; favorable overall response rate (ORR, confirmed or unconfirmed and ongoing) were seen both without prior chemo (50%) and with prior chemo (39%).
Responses were observed with or without concurrent T790M and with or without prior history of brain metastases
Robust C797S and T790M ctDNA clearance was observed in the context of diverse EGFR driver mutations including exon 19 del or indel, L858R, G719X, and exon20ins

Presentation Details
Abstract Title: First-in-human trial of BH-30643, a novel macrocyclic, non-covalent, mutant-selective OMNI-EGFR inhibitor, in EGFR-mutant (EGFRm) NSCLC
Abstract Number: 3014
Session Type/Title: Rapid Oral Abstract Session – Developmental Therapeutics​ – Molecularly Targeted Agents and Tumor Biology
Date and Time: June 2, 2026, at 9:45 AM – 11:15 AM CDT / 10:45 AM-12:15 PM EDT

About BH-30643
BH-30643 is an investigational, novel, orally bioavailable, non-covalent, macrocyclic, mutant-selective, OMNI-EGFR inhibitor. BH-30643 was designed to overcome the limitations of currently approved EGFR inhibitors, which were discovered over a decade ago without the current, modern understanding of the structure and protein dynamics of mutant EGFRs. In preclinical studies, BH-30643 demonstrated potent inhibitory activity across diverse EGFR mutation categories – classical activating mutations, on-target resistance mutations such as C797S with or without T790M, atypical mutations and exon 20 insertions – while maintaining marked selectivity over wild-type EGFR.

BH-30643 is currently being evaluated in the Phase 1/2 SOLARA clinical trial in adults with locally advanced or metastatic NSCLC harboring EGFR or HER2 mutations. For additional information on SOLARA, including a list of study sites and how to enroll, please visit clinicaltrials.gov (NCT06706076).

(Press release, BlossomHill Therapeutics, MAY 21, 2026, View Source [SID1234665993])

On May 21, 2026 HUTCHMED (China) Limited ("HUTCHMED") (Nasdaq/AIM:HCM; HKEX:13) and Innovent Biologics, Inc. ("Innovent", HKEX:1801) reported that the New Drug Application (NDA) for the combination of ELUNATE (fruquintinib) and TYVYT (sintilimab injection) has been granted approval by the China National Medical Products Administration ("NMPA") for the treatment of patients with locally advanced or metastatic renal cell carcinoma who have failed prior vascular endothelial growth factor receptor-tyrosine kinase inhibitors (VEGFR-TKI) therapy and have not received programmed death receptor-1 ("PD-1") or programmed death-ligand 1 ("PD-L1") inhibitor therapy in the first-line setting.

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The approval is supported by data from FRUSICA-2, a randomized, open-label, active-controlled registration study evaluating the efficacy and safety of fruquintinib in combination with sintilimab versus axitinib or everolimus monotherapy for the second-line treatment of patients with locally advanced or metastatic renal cell carcinoma. The study met its primary endpoint of progression free survival ("PFS") as assessed by blinded independent central review ("BICR").

"The rapid advancements in targeted therapies, immunotherapies, and their combination regimens have led to a significant evolution in the treatment landscape for advanced renal cell carcinoma. Optimizing the selection of treatment for individual patients is a key focus of clinical interest," said Professor Dingwei Ye of Fudan University Shanghai Cancer Center and co-lead Principal Investigator of the FRUSICA-2 study. "The approval of the fruquintinib and sintilimab combination underscores its potential to address the pressing medical needs of patients with this challenging disease."

"The FRUSICA-2 trial results provided compelling evidence that the fruquintinib and sintilimab combination could play a meaningful role in shaping second-line treatment strategies for advanced renal cell carcinoma," said Professor Zhisong He of Peking University First Hospital and co-lead Principal Investigator of the FRUSICA-2 study. "We are optimistic about the clinical implications of this approval as we strive to provide effective treatment options for patients."

"This approval reaffirms our deep commitment to delivering innovative therapies to patients facing advanced renal cell carcinoma in China, where second-line treatment options remain limited," said Mr Johnny Cheng, Acting Chief Executive Officer and Chief Financial Officer of HUTCHMED. "We are excited to continue pushing the boundaries of our research — across monotherapies, combination strategies, and exciting new platforms such as our ATTC technology — to unlock even greater therapeutic potential across various tumor types, ultimately providing more impactful and transformative solutions to patients."

Dr Hui Zhou, Chief R&D Officer of Oncology of Innovent, stated: "The approval is a significant milestone for patients with advanced renal cell carcinoma in China. It further validates the potential of the sintilimab plus fruquintinib combination regimen, now approved for two difficult-to-treat cancers. We are also proud to achieve the 10th approved indication for sintilimab (TYVYT), and remain committed to advancing clinical value optimization to benefit an even broader population of cancer patients."

About The FRUSICA-2 Trial

Results from the Phase III part of the study were presented at the 2025 European Society for Medical Oncology (ESMO) (Free ESMO Whitepaper) Congress. As of the PFS final analysis cutoff of February 17, 2025, the median follow-up was 16.6 months. The median PFS as assessed by BICR was 22.2 months with fruquintinib plus sintilimab, compared to 6.9 months with axitinib/everolimus (stratified hazard ratio [HR] 0.373; stratified log-rank p<0.0001). The objective response rate (ORR) was 60.5% vs 24.3% (Odds Ratio 4.622, p<0.0001), and the median duration of response (DoR) was 23.7 months vs 11.3 months, respectively. Overall survival data were still evolving at the time of data cutoff with maturity of approximately 20%. Efficacy benefits were observed in all prognostic risk groups, as defined by the International mRCC Database Consortium (IMDC) criteria. The safety profile of the fruquintinib and sintilimab combination was consistent with the known profiles of each individual treatment. Additional details may be found at clinicaltrials.gov, using identifier NCT05522231.

About Kidney Cancer and Renal Cell Carcinoma

It is estimated that approximately 435,000 new patients were diagnosed with kidney cancer worldwide in 2022.1 In China, an estimated 74,000 new patients were diagnosed with kidney cancer in 2022.2 Approximately 90% of kidney tumors are renal cell carcinoma.

About Fruquintinib

Fruquintinib is a selective oral inhibitor of all three vascular endothelial growth factor receptors ("VEGFR") -1, -2 and -3. VEGFR inhibitors play a pivotal role in inhibiting tumor angiogenesis. Fruquintinib was designed to have enhanced selectivity that limits off-target kinase activity, allowing for drug exposure that achieves sustained target inhibition and flexibility for potential use as part of a combination therapy.3

About Fruquintinib Approvals

Fruquintinib is co-developed and co-commercialized in China by HUTCHMED and Eli Lilly and Company under the brand name ELUNATE. It is approved for the treatment of patients with metastatic colorectal cancer who have previously received fluoropyrimidine, oxaliplatin and irinotecan-based chemotherapy, and those who have previously received or are not suitable to receive anti-VEGF therapy or anti-epidermal growth factor receptor (EGFR) therapy (RAS wild-type) in China. It was included in China’s National Reimbursement Drug List (NRDL) in January 2020.

The combination of ELUNATE (fruquintinib) and TYVYT (sintilimab injection) has conditional approval in China for the treatment of patients with advanced mismatch repair proficient (pMMR) endometrial cancer who have failed prior systemic therapy and are not candidates for curative surgery or radiation.

Takeda holds the exclusive worldwide license to further develop, commercialize, and manufacture fruquintinib outside mainland China, Hong Kong and Macau, marketing it under the brand name FRUZAQLA. Fruquintinib received approval for the treatment of previously treated metastatic colorectal cancer in the US, Europe, Japan and many other countries around the world.

About Sintilimab

Sintilimab, marketed as TYVYT (sintilimab injection) in China, is a PD-1 immunoglobulin G4 monoclonal antibody co-developed by Innovent and Eli Lilly and Company. Sintilimab is a type of immunoglobulin G4 monoclonal antibody, which binds to PD-1 molecules on the surface of T-cells, blocks the PD-1/PD-L1 pathway, and reactivates T-cells to kill cancer cells.

(Press release, Hutchison China MediTech, MAY 21, 2026, View Source [SID1234665930])

On May 21, 2026 Exelixis, Inc. (Nasdaq: EXEL) reported presentations for its flagship product, CABOMETYX (cabozantinib), and its investigational oral kinase inhibitor, zanzalintinib, at the 2026 American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting to be held from May 29 – June 2 in Chicago.

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"The presentations at ASCO (Free ASCO Whitepaper) this year highlight the continued progress of our strategy to build upon the well-established therapeutic profile of CABOMETYX and accelerate the development of zanzalintinib, our next oncology franchise molecule," said Dana T. Aftab, Ph.D., Executive Vice President, Research and Development, Exelixis. "New analyses from the phase 3 CABINET pivotal trial that further reinforce the foundational role of CABOMETYX in patient care, and findings from the phase 3 STELLAR-303 pivotal trial evaluating our investigational therapy, zanzalintinib, in metastatic colorectal cancer, will be presented. These collective data sets are a testament to our team’s dedication to improving the standards of care for patients with cancer."

Studies to be presented at the 2026 ASCO (Free ASCO Whitepaper) Annual Meeting include:

Abstract Title

Presentation

Session Title

Session Date/Time

Cabozantinib

A phase 2 randomized trial of radium-223 dichloride and cabozantinib in patients (pts) with renal cell carcinoma (RCC) with bone metastases (BM): RADICAL (Alliance A031801)

Oral Abstract #4500

Genitourinary Cancer – Kidney and Bladder

Friday, May 29
2:45 – 2:57 p.m. CDT

Interim analysis of CaboMain: A prospective, single-arm phase 2 clinical trial of cabozantinib as maintenance therapy for patients with "ultra-high-risk" pediatric solid tumors

Rapid Oral Abstract #10014

Pediatric Oncology II

Saturday, May 30
8:27 – 8:33 a.m. CDT

Efficacy and safety of cabozantinib (CABO) in advanced neuroendocrine tumors (NET) according to hormone functional status: Subgroup analysis of phase 3 CABINET trial (Alliance A021602)

Poster #161 Abstract #4178

Gastrointestinal Cancer – Gastroesophageal, Pancreatic and Hepatobiliary

Saturday, May 30
9:00 a.m. – 12:00 p.m. CDT

Cabozantinib in high-grade neuroendocrine neoplasms

Poster #166 Abstract #4183

Gastrointestinal Cancer – Gastroesophageal, Pancreatic and Hepatobiliary

Saturday, May 30
9:00 a.m. – 12:00 p.m. CDT

EA3231: A randomized phase 3 study of BRAF-targeted therapy vs cabozantinib in RAI-refractory differentiated thyroid cancer with BRAF V600Em

Poster #589b Abstract #TPS6140

Head and Neck Cancer

Saturday, May 30
1:30 – 4:30 p.m. CDT

Cabozantinib plus nivolumab (C+N) versus sunitinib (S) in patients with advanced renal cell carcinoma (aRCC) and bone metastasis: Updated subgroup analysis of the phase 3 CheckMate-9ER trial

Poster #7 Abstract #4528

Genitourinary Cancer – Kidney and Bladder

Sunday, May 31
9:00 a.m. – 12:00 p.m. CDT

Cabozantinib plus nivolumab (C+N) versus sunitinib (S) in patients with advanced renal cell carcinoma (aRCC) and liver metastasis: Subgroup analysis of the phase 3 CheckMate-9ER trial

Poster #9 Abstract

#4530

Genitourinary Cancer – Kidney and Bladder

Sunday, May 31
9:00 a.m. – 12:00 p.m. CDT

PEMBROCABOSARC: A phase 2 trial combining pembrolizumab and cabozantinib in patients with advanced undifferentiated pleomorphic sarcoma

Rapid Oral Abstract

#11514

Sarcoma

Sunday, May 31
4:42 – 4:48 p.m. CDT

MAIN-CAV: Phase 3 randomized trial of maintenance cabozantinib and avelumab versus avelumab after first-line platinum-based chemotherapy (PBC) in patients (pts) with locally advanced/metastatic urothelial cancer (la/mUC; Alliance A032001)

Rapid Oral Abstract #4514

Genitourinary Cancer – Kidney and Bladder

Monday, June 1
8:00 – 8:06 a.m. CDT

Final results of a phase 2 trial of cabozantinib plus nivolumab (CaboNivo) in patients with non-clear cell renal cell carcinoma (nccRCC)

Rapid Oral Abstract

#4521

Genitourinary Cancer – Kidney and Bladder

Monday, June 1
9:12 – 9:18 a.m. CDT

Survival outcomes of cabozantinib treatment with and without immune checkpoint inhibition in patients with heavily pretreated advanced sarcoma

Poster #341 Abstract #11551

Sarcoma

Monday, June 1
1:30 – 4:30 p.m. CDT

Safety and feasibility of cabozantinib (CABO) in combination with cisplatin, doxorubicin, and high-dose methotrexate (MAP) in patients with newly diagnosed high-risk osteosarcoma (OS)

Poster #281 Abstract #10030

Pediatric Oncology

Monday, June 1
1:30 – 4:30 p.m. CDT

Zanzalintinib

Contribution of atezolizumab (atezo) to the efficacy of the zanzalintinib (zanza) + atezo combination in patients (pts) with previously treated metastatic colorectal cancer (mCRC): Evidence from the phase 3 STELLAR-303 trial

Poster #341 Abstract #3574

Gastrointestinal Cancer – Colorectal and Anal

Saturday, May 30
9:00 a.m. – 12:00 p.m. CDT

ZAMBONI: A phase 2 study of zanzalintinib for metastatic clear cell renal cell carcinoma with bone metastases previously treated with immune checkpoint inhibitors

Poster #110b Abstract #TPS4634

Genitourinary Cancer – Kidney and Bladder

Sunday, May 31
9:00 a.m. – 12:00 p.m. CDT

A phase 2 trial of neoadjuvant zanzalintinib (ZANZA) plus nivolumab (NIVO) in patients with locally advanced and/or surgically challenging clear cell renal cell carcinoma (EXPLORE-RCC)

Poster #108a Abstract

#TPS4629

Genitourinary Cancer – Kidney and Bladder

Sunday, May 31
9:00 a.m. – 12:00 p.m. CDT

LITESPARK-033: Phase 3 study of belzutifan plus zanzalintinib versus cabozantinib for recurrent clear cell renal cell carcinoma during or after adjuvant anti-PD-(L)1 therapy

Poster #110a Abstract #TPS4633

Genitourinary Cancer – Kidney and Bladder

Sunday, May 31
9:00 a.m. – 12:00 p.m. CDT

About CABOMETYX (cabozantinib)
In the U.S., CABOMETYX tablets are approved as monotherapy for the treatment of patients with advanced RCC and in combination with nivolumab as a first-line treatment for patients with advanced RCC; for the treatment of patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib; for adult and pediatric patients 12 years of age and older with locally advanced or metastatic differentiated thyroid cancer (DTC) that has progressed following prior VEGFR-targeted therapy and who are radioactive iodine-refractory or ineligible; for the treatment of adult and pediatric patients 12 years of age and older with previously treated, unresectable, locally advanced or metastatic, well-differentiated pancreatic NET; and adult and pediatric patients 12 years of age and older with previously treated, unresectable, locally advanced or metastatic, well-differentiated extra-pancreatic NET. CABOMETYX tablets have also received regulatory approvals in over 65 countries outside the U.S. and Japan, including the EU. In 2016, Exelixis granted Ipsen Pharma SAS exclusive rights for the commercialization and further clinical development of cabozantinib outside of the U.S. and Japan. In 2017, Exelixis granted exclusive rights to Takeda Pharmaceutical Company Limited for the commercialization and further clinical development of cabozantinib for all future indications in Japan. Exelixis holds the exclusive rights to develop and commercialize cabozantinib in the U.S.

IMPORTANT SAFETY INFORMATION

WARNINGS AND PRECAUTIONS

Hemorrhage: CABOMETYX can cause severe and fatal hemorrhages. The incidence of Grade 3-5 hemorrhagic events was 5% in CABOMETYX patients in RCC, HCC, and DTC studies. Discontinue CABOMETYX for Grade 3-4 hemorrhage and before surgery. Do not administer to patients who have a recent history of hemorrhage, including hemoptysis, hematemesis, or melena.

Perforations and Fistulas: Fistulas, including fatal cases, and gastrointestinal (GI) perforations, including fatal cases, each occurred in 1% of CABOMETYX patients. Monitor for signs and symptoms, and discontinue CABOMETYX in patients with Grade 4 fistulas or GI perforation.

Thromboembolic Events: CABOMETYX can cause arterial or venous thromboembolic events. Venous thromboembolism occurred in 7% (including 4% pulmonary embolism) and arterial thromboembolism in 2% of CABOMETYX patients. Fatal thrombotic events have occurred. Discontinue CABOMETYX in patients who develop an acute myocardial infarction or serious arterial or venous thromboembolic events.

Hypertension and Hypertensive Crisis: CABOMETYX can cause hypertension, including hypertensive crisis. Hypertension was reported in 37% (16% Grade 3 and <1% Grade 4) of CABOMETYX patients. In CABINET (n=195), hypertension occurred in 65% (26% Grade 3) of CABOMETYX patients. Do not initiate CABOMETYX in patients with uncontrolled hypertension. Monitor blood pressure regularly during CABOMETYX treatment. Withhold CABOMETYX for hypertension that is not adequately controlled; when controlled, resume at a reduced dose. Permanently discontinue CABOMETYX for severe hypertension that cannot be controlled with antihypertensive therapy or for hypertensive crisis.

Cardiac Failure: CABOMETYX can cause severe and fatal cardiac failure. Cardiac failure occurred in 0.5% of patients treated with CABOMETYX as a single agent, including fatal cardiac failure in 0.1% of patients. Consider baseline and periodic evaluations of left ventricular ejection fraction. Monitor for signs and symptoms of cardiovascular events. Withhold and resume at a reduced dose upon recovery or permanently discontinue depending on the severity.

Diarrhea: CABOMETYX can cause diarrhea and it occurred in 62% (10% Grade 3) of treated patients. Monitor and manage patients using antidiarrheals as indicated. Withhold CABOMETYX until improvement to ≤ Grade 1; resume at a reduced dose.

Palmar-Plantar Erythrodysesthesia (PPE): CABOMETYX can cause PPE and it occurred in 45% of treated patients (13% Grade 3). Withhold CABOMETYX until PPE resolves or decreases to Grade 1 and resume at a reduced dose for intolerable Grade 2 PPE or Grade 3 PPE.

Hepatotoxicity: CABOMETYX in combination with nivolumab in RCC can cause hepatic toxicity with higher frequencies of Grades 3 and 4 ALT and AST elevations compared to CABOMETYX alone. With the combination of CABOMETYX and nivolumab, Grades 3 and 4 increased ALT or AST were seen in 11% of patients. Monitor liver enzymes before initiation of treatment and periodically. Consider more frequent monitoring as compared to when the drugs are administered as single agents. Consider withholding CABOMETYX and/or nivolumab, initiating corticosteroid therapy, and/or permanently discontinuing the combination for severe or life-threatening hepatotoxicity.

Adrenal Insufficiency: CABOMETYX in combination with nivolumab can cause primary or secondary adrenal insufficiency. Adrenal insufficiency occurred in 4.7% (15/320) of patients with RCC who received CABOMETYX with nivolumab, including Grade 3 (2.2%), and Grade 2 (1.9%) adverse reactions. Withhold CABOMETYX and/or nivolumab and resume CABOMETYX at a reduced dose depending on severity.

Proteinuria: Proteinuria was observed in 8% of CABOMETYX patients. Monitor urine protein regularly during CABOMETYX treatment. For Grade 2 or 3 proteinuria, withhold CABOMETYX until improvement to ≤ Grade 1 proteinuria; resume CABOMETYX at a reduced dose. Discontinue CABOMETYX in patients who develop nephrotic syndrome.

Osteonecrosis of the Jaw (ONJ): CABOMETYX can cause ONJ and it occurred in <1% of treated patients. Perform an oral examination prior to CABOMETYX initiation and periodically during treatment. Advise patients regarding good oral hygiene practices. Withhold CABOMETYX for at least 3 weeks prior to scheduled dental surgery or invasive dental procedures. Withhold CABOMETYX for development of ONJ until complete resolution; resume at a reduced dose.

Impaired Wound Healing: CABOMETYX can cause impaired wound healing. Withhold CABOMETYX for at least 3 weeks prior to elective surgery. Do not administer for at least 2 weeks after major surgery and until adequate wound healing. The safety of resumption of CABOMETYX after resolution of wound healing complications has not been established.

Reversible Posterior Leukoencephalopathy Syndrome (RPLS): CABOMETYX can cause RPLS. Perform evaluation for RPLS and diagnose by characteristic finding on MRI any patient presenting with seizures, headache, visual disturbances, confusion, or altered mental function. Discontinue CABOMETYX in patients who develop RPLS.

Thyroid Dysfunction: CABOMETYX can cause thyroid dysfunction, primarily hypothyroidism, and it occurred in 19% of treated patients (0.4% Grade 3). Assess for signs of thyroid dysfunction prior to the initiation of CABOMETYX and monitor for signs and symptoms during treatment.

Hypocalcemia: CABOMETYX can cause hypocalcemia, with the highest incidence in DTC patients. Based on the safety population, hypocalcemia occurred in 13% of CABOMETYX patients (2% Grade 3 and 1% Grade 4).

Monitor blood calcium levels and replace calcium as necessary during treatment. Withhold and resume CABOMETYX at a reduced dose upon recovery or permanently discontinue CABOMETYX depending on severity.

Embryo-Fetal Toxicity: CABOMETYX can cause fetal harm. Advise pregnant women of the potential risk to a fetus and advise females of reproductive potential to use effective contraception during treatment with CABOMETYX and for 4 months after the last dose.

ADVERSE REACTIONS

The most common (≥20%) adverse reactions are:

CABOMETYX as a single agent: diarrhea, fatigue, PPE, decreased appetite, hypertension, nausea, vomiting, weight decreased, and constipation.

CABOMETYX in combination with nivolumab: diarrhea, fatigue, hepatotoxicity, PPE, stomatitis, rash, hypertension, hypothyroidism, musculoskeletal pain, decreased appetite, nausea, dysgeusia, abdominal pain, cough, and upper respiratory tract infection.

DRUG INTERACTIONS

Strong CYP3A4 Inhibitors: If coadministration with strong CYP3A4 inhibitors cannot be avoided, reduce the CABOMETYX dosage. Avoid grapefruit or grapefruit juice.

Strong or Moderate CYP3A4 Inducers: If coadministration with strong or moderate CYP3A4 inducers cannot be avoided, increase the CABOMETYX dosage. Avoid St. John’s wort.

USE IN SPECIFIC POPULATIONS

Lactation: Advise women not to breastfeed during CABOMETYX treatment and for 4 months after the final dose.

Hepatic Impairment: In patients with moderate hepatic impairment, reduce the CABOMETYX dosage. Avoid CABOMETYX in patients with severe hepatic impairment.

Pediatric Use: Physeal widening has been observed in children with open growth plates when treated with CABOMETYX. Physeal and longitudinal growth monitoring is recommended in children (12 years and older) with open growth plates. Consider interrupting or discontinuing CABOMETYX if abnormalities occur. The safety and effectiveness of CABOMETYX in pediatric patients less than 12 years of age have not been established.

Please see accompanying full Prescribing Information View Source

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.FDA.gov/medwatch or call 1-800-FDA-1088.

About Zanzalintinib
Zanzalintinib is a novel oral kinase inhibitor that inhibits the activity of the TAM kinases (TYRO3, AXL, MER), MET and VEGF receptors. These kinases play important roles in oncogenic processes, including tumor cell proliferation, metastasis, angiogenesis, drug resistance and evasion of antitumor immunity. The zanzalintinib development program includes a series of ongoing and planned pivotal trials to explore its therapeutic potential in CRC, clear cell and non-clear cell RCC, and NET, as well as earlier-stage trials in meningioma, lung cancer and castration-resistant prostate cancer.

In February 2026, Exelixis announced that the U.S. Food and Drug Administration (FDA) accepted the company’s New Drug Application for zanzalintinib, in combination with atezolizumab (Tecentriq), for the treatment of adult patients with mCRC who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, and, if RAS wild-type, an anti-epidermal growth factor receptor (EGFR) therapy. The FDA assigned a Prescription Drug User Fee Act target action date of December 3, 2026.

Zanzalintinib is an investigational agent that is not approved for any use and is the subject of ongoing clinical trials.

(Press release, Exelixis, MAY 21, 2026, View Source [SID1234665946])

On May 21, 2026 Accent Therapeutics, a clinical-stage biopharmaceutical company pioneering novel small molecule precision cancer therapies, reported it will present a Trial in Progress poster describing its ongoing Phase 1/2 first-in-human clinical study of ATX-295 at the 2026 American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting, taking place May 29 – June 2 in Chicago, Illinois.

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"KIF18A inhibition offers a differentiated approach to exploiting a fundamental vulnerability in chromosomally instable tumors including high grade serous ovarian cancer (HGSOC) and squamous non-small cell lung cancer (sqNSCLC). ATX-295 is grounded in a strong body of preclinical evidence that continues to deepen our conviction in this program," said Jason Sager, M.D., Chief Medical Officer of Accent Therapeutics. "We have built a rigorous clinical development plan focused on treating cancers with high unmet need, and we hope to ultimately deliver a meaningful new targeted oncology option for patients with limited therapeutic alternatives."

ATX-295 is a potentially best-in-class inhibitor of KIF18A, a mitotic kinesin motor protein critical for cell division in select tumors with chromosomal instability.

The Trial in Progress poster will describe the design and scientific rationale for Accent’s first-in-human Phase 1/2 dose-escalation and expansion study evaluating the safety, tolerability, and preliminary efficacy of ATX-295 in patients with locally advanced or metastatic solid tumors (NCT06799065), including HGSOC and sqNSCLC.

The study comprises an initial dose-escalation phase to determine the recommended Phase 2 dose (RP2D), followed by a dose-expansion phase to assess preliminary antitumor activity. Primary endpoints include evaluation of the safety and tolerability of ATX-295 and determination of the RP2D. Secondary endpoints include assessment of pharmacokinetics (PK), pharmacodynamic (PD) effects, and preliminary antitumor activity. The Phase 1/2 study is currently open and actively enrolling patients.

Details for the presentation are as follows:

Poster Title: Trial in Progress: A Phase 1/2 First-in-Human Study of ATX-295, an Oral Inhibitor of KIF18A, in Patients with Advanced or Metastatic Solid Tumors, Including Ovarian Cancer
Abstract Number: TPS3167
Session Title: Developmental Therapeutics—Molecularly Targeted Agents and Tumor Biology
Session Date and Time: Saturday, May 30, 1:30 – 4:30 PM CDT
Location: Hall A – Posters and Exhibits
Presenter: Judy S. Wang, MD, Florida Cancer Specialists/Sarah Cannon Research Institute
The poster will be available on the Accent Therapeutics website following the meeting.

About ATX-295
Accent’s lead program, ATX-295, is a potential best-in-class inhibitor for KIF18A, a mitotic kinesin motor protein critical for cell division in select tumors with chromosomal instability. KIF18A inhibitor treatment results in rapid cell death for cancers with an abnormal number of chromosomes (aneuploid) in vitro and in vivo, while cells with normal numbers of chromosomes (euploid) are unaffected. ATX-295 may address a large patient population across several cancer indications, including ovarian and squamous non-small cell lung cancer. Accent retains full worldwide rights to the KIF18A program, currently being evaluated in an ongoing Phase 1/2 clinical study (NCT06799065) enrolling patients with locally advanced or metastatic solid tumors, including high-grade serous ovarian cancer and squamous non-small cell lung cancer.

(Press release, Accent Therapeutics, MAY 21, 2026, View Source [SID1234665962])