NCT05047536

KZR-261 in Subjects With Advanced Solid Malignancies

A Phase 1 Study of KZR-261, a Small Molecule Sec61 Inhibitor, in Subjects With Advanced Solid Malignancies

• Status: Terminated
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 61 (actual)
• Sponsor: Kezar Life Sciences, Inc. · Industry
• Sex: All
• Age: 18 Years
• Healthy volunteers: Not accepted

Summary

A first-in-human, open-label, multicenter, Phase 1 study of KZR-261 designed to assess the safety and tolerability, preliminary anti-tumor activity, and pharmacokinetics (PK) of KZR-261, as well as identify the recommended Phase 2 dose (RP2D). The study comprised a Part 1 (Dose Escalation) and a Part 2 (2A Dose Expansion and 2B Dose Optimization) in solid organ tumors (melanoma/uveal melanoma, mesothelioma, colorectal cancer, castration-resistant prostate cancer, and "All-Tumors").

Detailed description

The first-in-human, open-label, multicenter, Phase 1 study of KZR-261, Study KZR-261-101, was conducted in two parts (dose escalation and dose expansion) to evaluate the safety and tolerability, pharmacokinetics, pharmacodynamics, and evaluate the preliminary anti-tumor activity of KZR-261 in participants with locally advanced or metastatic solid malignancies for whom no therapeutics are available (or available therapeutics were refused) that can confer a reasonable likelihood of clinical benefit. The 5 tumor cohorts in the dose expansion part include advanced malignant: * melanoma/uveal melanoma * mesothelioma * colorectal cancer * castration-resistant prostate cancer * "All-Tumors" (other advanced solid malignancies) Part 1 (Dose Escalation) and Part 2 (2A Dose Expansion and 2B Dose Optimization) comprised a 4-week Screening Period, a Treatment Period lasting approximately 24 weeks, 4-6-week Safety Follow-up, and a 12-month Long-Term Follow-up Period (after last dose of study treatment), for a total study duration of approximately 20 months.

Conditions

• Advanced/Metastatic Solid Tumor

Interventions

Type	Name	Description
DRUG	KZR-261	KZR-261 for Injection is a lyophilized drug product supplied in single-use vials delivering 75 mg of KZR-261.

Timeline

• Start date: 2021-09-30
• Primary completion: 2025-01-17
• Completion: 2025-01-17
• First posted: 2021-09-17
• Last updated: 2025-12-19
• Results posted: 2025-12-19

Locations

12 sites across 1 country: United States

Regulatory

• FDA-regulated drug study