Zanzalintinib

Phase 3Small molecule

Zanzalintinib is one of 379 small molecule programs targeting Metastatic Castration-Resistant Prostate Cancer. It is currently in Phase 3.

Indications

Total Trials

Active Trials

378

Competitors

Pipeline

Status by Indication[3][1]

Indication

Metastatic Castration-Resistant Prostate CancerNot yet recruiting

Renal Cell Carcinoma (RCC)Enrolling by invitation

Solid TumorRecruiting

Advanced Hepatocellular CarcinomaRecruiting

Differentiated Thyroid Gland CarcinomaRecruiting

Colon Cancer MetastaticNot yet recruiting

Adenoid Cystic CarcinomaNot yet recruiting

PheochromocytomaNot yet recruiting

Pancreatic Neuroendocrine TumorRecruiting

Clear Cell Renal Cell CarcinomaNot yet recruiting

Metastatic Castration-Resistant Prostate CancerPhase 2

Not yet recruiting

Renal Cell Carcinoma (RCC)Phase 3

Enrolling by invitation

Solid TumorPhase 1

Recruiting

Advanced Hepatocellular CarcinomaPreclinical

Recruiting

Differentiated Thyroid Gland CarcinomaPhase 2

Recruiting

Colon Cancer MetastaticPhase 2

Not yet recruiting

Adenoid Cystic CarcinomaPhase 2

Not yet recruiting

PheochromocytomaPhase 2

Not yet recruiting

Pancreatic Neuroendocrine TumorPreclinical

Recruiting

Clear Cell Renal Cell CarcinomaPhase 2

Not yet recruiting

Showing 10 of 32 indications

Competition

Competitive Landscape

348 competitors in Solid Tumor

#DrugCompanyPhaseTrials

Zanzalintinib

Merck & Co.

Phase 3

1 2

DATROWAY

Daiichi Sankyo

Preclinical

1 3

Fludara

Sanofi

Preclinical

1 4

Sporanox

SSebela Pharmaceuticals Development LLC

Preclinical

2 5

Augtyro

KKaruna Therapeutics, Inc., a Bristol Myers Squibb company

Preclinical

2 6

Paxil

SSebela Pharmaceuticals Development LLC

Preclinical

1 7

Navmi

SSummit Therapeutics

Preclinical

1 8

PD-1 Inhibitor

Johnson & Johnson

Preclinical

1 9

Tulmimetostat

Novartis

Preclinical

1 10

Chemotherapy Drug

Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Preclinical

Ranked by pipeline maturity and clinical activity. Current drug highlighted in teal.

Timeline

Expected Milestones

Q2 2027

Phase 2Recruiting

Hepatocellular Carcinoma

NCT06698250

Phase 1Recruiting

Pembrolizumab

NCT06912087

Q3 2027

Phase 2Not yet recruiting

Hepatocellular Cancer

NCT07226063

Q4 2027

Phase 1Recruiting

Solid Tumor

NCT06952010

Q3 2028

Phase 1Not yet recruiting

Pediatric Cancer

NCT07773454

Clinical

Trials by Indication[1]

Renal Cell Carcinoma3 trials

Study of Zanzalintinib (XL092) + AB521 and Zanzalintinib + AB521 + Nivolumab in Participants With Advanced Clear Cell Renal Cell Carcinoma (ccRCC) or Other Advanced Solid Tumors (STELLAR-009)

Terminated·EExelixis·Phase 1·NCT06191796·25 enrolled

A Phase 1b/2 Study of Immune and Targeted Combination Therapies in Participants With RCC (KEYMAKER-U03): Substudy 03C in Participants With Recurrent Disease During or After Anti-PD-(L)1 Adjuvant Therapy

Recruiting· Merck & Co. logo

Merck & Co.·Preclinical·NCT07049926·140 enrolled

A Phase 3, Randomized, Open-label Study of Belzutifan + Zanzalintinib Versus Cabozantinib in Participants With Advanced RCC Who Experienced Disease Recurrence During or After Prior Adjuvant Anti-PD-1/L1 Therapy (LITESPARK-033)

Recruiting· Merck & Co. logo

Merck & Co.·Phase 3·NCT07227402·904 enrolled

Leiomyosarcoma2 trials

XL092 (Zanzalintinib) for the Treatment of Patients With Metastatic or Unresectable Leiomyosarcoma

Recruiting·NNorthwestern University·Phase 2·NCT06571734·29 enrolled

Zanzalintinib Combined With Eribulin in Advanced Liposarcoma and Leiomyosarcoma

Recruiting·WWashington University School of Medicine·Phase 1·NCT06957431·18 enrolled

Renal Cell Carcinoma (RCC)2 trials

Long-Term Extension Study for Participants Previously Enrolled in an Exelixis-Sponsored Study

Enrolling by invitation·EExelixis·Phase 3·NCT07620574·5,000 enrolled

A Dose-Escalation and Expansion Study of the Safety and Efficacy of XL092 in Combination With Immuno-Oncology or Other Agents in Subjects With Unresectable Advanced or Metastatic Solid Tumors

Recruiting·EExelixis·Phase 1·NCT05176483·1,394 enrolled

Head and Neck Squamous Cell Carcinoma1 trial

Study of Zanzalintinib (XL092) + Pembrolizumab vs Pembrolizumab in Subjects With PD-L1 Positive Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma

Active, not recruiting·EExelixis·Phase 2/3·NCT06082167·600 enrolled

Pembrolizumab1 trial

Dose Finding Study of Zanzalintinib With Pembrolizumab and Cetuximab in Head and Neck SCC

Recruiting·UUniversity of Chicago·Phase 1·NCT06912087·36 enrolled

29 more indications

AIN1 trial

Maintenance Zanzalintinib With Etoposide After HDCT in GCT

Recruiting·IIndiana University·Phase 1/2·NCT06937866·38 enrolled

Uterine Cancer1 trial

Zanzalintinib in Combination With Paclitaxel in Recurrent High Grade Uterine Cancer

Recruiting·WWashington University School of Medicine·Phase 1·NCT06795009·36 enrolled

Neuroendocrine Neoplasm1 trial

Zanzalintinib Maintenance in Patients With High Grade Neuroendocrine Neoplasms (HG-NENs)

Recruiting·WWashington University School of Medicine·Phase 2·NCT06926634·32 enrolled

Hepatocellular Cancer1 trial

Maintenance Zanzalintinib and Durvalumab in Participants With Advanced Hepatocellular Cancer

Not yet recruiting·AAmit Mahipal·Phase 2·NCT07226063·16 enrolled

Moderate Hepatic Impairment1 trial

Pharmacokinetics (PK) and Safety of Zanzalintinib in Participants With Moderate Hepatic Impairment (HI)

Recruiting·EExelixis·Phase 1·NCT06962332·20 enrolled

Hepatocellular Carcinoma1 trial

Zanzalintinib (XL-092) Plus Durvalumab and Tremelimumab in Unresectable Hepatocellular Carcinoma (ZENOBIA)

Recruiting·AAnwaar Saeed·Phase 2·NCT06698250·40 enrolled

Carcinoma, Renal Cell1 trial

A Phase 3, Randomized, Double-blind, Study of Belzutifan + Zanzalintinib Versus Belzutifan + Placebo in Participants With Advanced RCC Who Have Progressed on or After Both PD-1/L1 and VEGF-TKI Therapies in Sequence or in Combination (LITESPARK-034)

Recruiting· Merck & Co. logo

Merck & Co.·Phase 3·NCT07489495·758 enrolled

Metastatic Castration-Resistant Prostate Cancer1 trial

A Single Arm Phase II Trial of Zanzalitinib in Patients With Metastatic Castration Resistant Prostate Cancer (mCRPC) With Soft Tissue or Visceral Metastases

Not yet recruiting·PPedro Barata, MD, MSc·Phase 2·NCT07608718·19 enrolled

Pancreatic Neuroendocrine Tumor1 trial

A Phase 2/3, Multicenter, Randomized Open-Label Study of Zanzalintinib vs Everolimus in Participants With Previously Treated, Unresectable, Locally Advanced or Metastatic Neuroendocrine Tumors

Recruiting·EExelixis·Preclinical·NCT06943755·440 enrolled

Meningioma1 trial

A Phase 2, Single-Arm, Multicenter, Open-Label Study of Zanzalintinib in Participants With Recurrent or Progressive Meningioma

Recruiting·EExelixis·Phase 2·NCT07428616·100 enrolled

Locally Advanced Renal Cell Carcinoma1 trial

A Phase II, Open-label, Single-arm Study of nEoadjuvant Zanzalintinib (XL092) Plus nivoLumab in Patients With lOcally Advanced and/or inopeRable clEar Cell Renal Cell Carcinoma With or Without Non-measurable Metastasis (EXPLORE-RCC)

Recruiting·QQian Qin·Phase 2·NCT06794229·69 enrolled

Neoadjuvant Treatment1 trial

ZAnzalintinib Neoadjuvant EValuation in Thyroid Oncology (ZANEVO)

Recruiting·MM.D. Anderson Cancer Center·Phase 2·NCT06959511·45 enrolled

Metastatic Soft-tissue Sarcoma1 trial

Phase I Study With Expansion Cohort of Zanzalintinib in Combination With Ipilimumab and Nivolumab in Patients With Metastatic Soft Tissue Sarcoma

Suspended·WWashington University School of Medicine·Phase 1·NCT06968988·18 enrolled

Advanced Urothelial Carcinoma1 trial

Phase II Trial of Zanzalintinib for Advanced Urothelial Carcinoma Progressing After Prior Therapy

Not yet recruiting·GGuru Sonpavde·Phase 2·NCT07185945·44 enrolled

Aggressive Variant Prostate Carcinoma1 trial

Phase II Study of Zanzalintinib in Men With Aggressive Variant Prostate Cancer (NAPOLEON Study)

Recruiting·DDeepak Kilari·Phase 2·NCT07218666·30 enrolled

Colorectal Cancer1 trial

Randomized Phase 3 Study of Zanzalintinib ± Subcutaneous Pembrolizumab and Berahyaluronidase Alfa (MK-3475A) Versus Placebo in Participants With Colorectal Cancer With Stage II/III Molecular Residual Disease Following Definitive Therapy

Not yet recruiting·EExelixis·Phase 3·NCT07750158·600 enrolled

Zanzalintinib1 trial

Phase 2 Trial of Zanzalintinib and Pembrolizumab in Select Subtypes of Advanced/Metastatic Soft-tissue Sarcoma

Recruiting·MM.D. Anderson Cancer Center·Phase 2·NCT07283731·20 enrolled

Pediatric Cancer1 trial

A Phase 1 Dose-Escalation Study of XL092 in Children and Adolescents With Relapsed or Refractory Solid Tumors

Not yet recruiting·EExelixis·Phase 1·NCT07773454·18 enrolled

Metastatic Olfactory Neuroblastoma1 trial

A Phase 2 Study Of Zanzalintinib For Patients With Recurrent Or Metastatic Olfactory Neuroblastoma

Not yet recruiting·MM.D. Anderson Cancer Center·Phase 2·NCT07527169·16 enrolled

Anaplastic Thyroid Cancer1 trial

A Multi-Center Single-Arm Phase 2 Trial Of Zanzalintinib In Combination With Cemiplimab In BRAF Wild-Type Anaplastic Thyroid Cancer: The ZEPHYR Trial

Not yet recruiting·MM.D. Anderson Cancer Center·Phase 2·NCT07470489·12 enrolled

Clear Cell Renal Cell Cancer (ccRCC)1 trial

A Phase II Study of Zanzalintinib for Metastatic Clear Cell Renal Cell Carcinoma With Bone Metastases in Patients Previously Treated With Immune Checkpoint Inhibitors

Recruiting·KKelly Fitzgerald, MD·Phase 2·NCT07043608·20 enrolled

Pheochromocytoma1 trial

A Phase 2 Clinical Trial of Zanzalintinib in Patients With Unresectable and Progressive Metastatic Pheochromocytoma or Paraganglioma (MPPGs)

Not yet recruiting·DDana-Farber Cancer Institute·Phase 2·NCT07714551·14 enrolled

Clear Cell Renal Cell Carcinoma1 trial

A Phase 2 Multicenter Single-Arm Clinical Trial of Zanzalintinib and Pembrolizumab in Subjects With Resectable Clear Cell Renal Cell Carcinoma

Not yet recruiting·YYonsei University·Phase 2·NCT07691476·48 enrolled

Adenoid Cystic Carcinoma1 trial

ZANACC: Phase 2 Non-randomized Single Arm Study Evaluating Zanzalintinib in Patients With Recurrent or Metastatic Adenoid Cystic Carcinoma of the Head and Neck

Not yet recruiting·UUNICANCER·Phase 2·NCT07682675·51 enrolled

Colon Cancer Metastatic1 trial

NIMBLE-CRC: NeoImmunoModulation Before Leveraging Excision in Colorectal Rectal Cancer

Not yet recruiting·NNorthwell Health·Phase 2·NCT07677579·26 enrolled

Differentiated Thyroid Gland Carcinoma1 trial

A Phase 2 Open Label Study of XL092 as First Line Therapy in Radioiodine Refractory Differentiated Thyroid Cancer

Recruiting·NNorthwestern University·Phase 2·NCT06959641·33 enrolled

Advanced Hepatocellular Carcinoma1 trial

A Phase Ib/II Study of Zanzalintinib in Second Line and Beyond for the Treatment of Advanced Hepatocellular Carcinoma

Recruiting·NNorthwestern University·Preclinical·NCT07042919·59 enrolled

Solid Tumor1 trial

A Phase 1 Dose Escalation and Expansion Study of XB628 as a Single Agent and in Combination With Zanzalintinib in Participants With Advanced or Metastatic Solid Tumors

Recruiting·EExelixis·Phase 1·NCT06952010·303 enrolled

Bone Sarcoma1 trial

A Phase 2 Trial of Zanzalintinib in Advanced/Metastatic Bone Sarcomas (ZAMBONE)

Recruiting·MM.D. Anderson Cancer Center·Phase 2·NCT07193550·70 enrolled

Sources

References

[1]
ClinicalTrials.gov — 38 trial records for Zanzalintinib. U.S. National Library of Medicine, National Institutes of Health.
[2]
ChEMBL — Zanzalintinib compound record. European Bioinformatics Institute (EMBL-EBI).
[3]
Open Targets Platform — Drug–disease associations for Zanzalintinib. EMBL-EBI & Wellcome Sanger Institute.
[4]
SEC EDGAR — Merck & Co. company filings. U.S. Securities and Exchange Commission.

Details

Drug Info

Quick Facts

Modality: Small molecule[2]
Highest Phase: Phase 3[1]
Company: Merck & Co.

Zanzalintinib

Status by Indication[3][1]

Competitive Landscape

Expected Milestones

Q2 2027

Q3 2027

Q4 2027

Q3 2028

Trials by Indication[1]

Renal Cell Carcinoma3 trials

Leiomyosarcoma2 trials

Renal Cell Carcinoma (RCC)2 trials

Head and Neck Squamous Cell Carcinoma1 trial

Pembrolizumab1 trial

AIN1 trial

Uterine Cancer1 trial

Neuroendocrine Neoplasm1 trial

Hepatocellular Cancer1 trial

Moderate Hepatic Impairment1 trial

Hepatocellular Carcinoma1 trial

Carcinoma, Renal Cell1 trial

Metastatic Castration-Resistant Prostate Cancer1 trial

Pancreatic Neuroendocrine Tumor1 trial

Meningioma1 trial

Locally Advanced Renal Cell Carcinoma1 trial

Neoadjuvant Treatment1 trial

Metastatic Soft-tissue Sarcoma1 trial

Advanced Urothelial Carcinoma1 trial

Aggressive Variant Prostate Carcinoma1 trial

Colorectal Cancer1 trial

Zanzalintinib1 trial

Pediatric Cancer1 trial

Metastatic Olfactory Neuroblastoma1 trial

Anaplastic Thyroid Cancer1 trial

Clear Cell Renal Cell Cancer (ccRCC)1 trial

Pheochromocytoma1 trial

Clear Cell Renal Cell Carcinoma1 trial

Adenoid Cystic Carcinoma1 trial

Colon Cancer Metastatic1 trial

Differentiated Thyroid Gland Carcinoma1 trial

Advanced Hepatocellular Carcinoma1 trial

Solid Tumor1 trial

Bone Sarcoma1 trial

References

Drug Info

Quick Facts

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