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Zumsemetinib

Phase 1

Hormone Receptor Positive HER-2 Negative Metastatic Breast Cancer | Small molecule | Oncology |Aclaris Therapeutics, Inc.|Last Updated: Apr 20, 2026

Success Probability
Approval Probability 71%
TA Base Rate26%
Adjusted LOA41%
ML RiskLOW_RISK
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Market & Valuation
rNPV $3.2B
Market Size $9.4B
Revenue Basis $1.6B
Competitors 6
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Trial Design
RandomizedACTIVE_CONTROLLEDDMCBiomarker
Total Trials1
Total Enrollment152
FDA Designations
No designations recorded
Clinical Trials (1)
NCT IDTitlePhaseStatusEnrollmentVelocityDesignStartCompletionLast UpdatedSitesCountries
NCT06374459Zunsemetinib in Combination With Capecitabine in Patients With Hormone Receptor-Positive and HER2-Negative Metastatic Breast Cancer With Bone MetastasisPHASE1 RECRUITING 152Jan 30, 2025May 31, 2032Apr 20, 20263 United States
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Study Endpoints
Primary Endpoints
Number of participants with adverse events (Phase Ib only)
From start of treatment through 30 days after end of treatment (estimated to be 11 months)
Recommended phase II dose of zunsemetinib (Phase Ib only)
Through end of 1st cycle (each cycle is 21 days)
Number of participants with dose-limiting toxicities (Phase Ib only)
Through end of 1st cycle (each cycle is 21 days)
Percent change in serum CTX (Phase II only)
Baseline and Day 1 of week 7
Progression-free survival (PFS) (Phase II only)
From start of treatment through completion of follow-up (estimated to be 3 years and 10 months)
Secondary Endpoints
Treatment-induced changes in DEXA BMD (g/cm^2) at hip and spine (Phase Ib only)
Baseline, end of cycle 8 (each cycle is 21 days), and end of treatment (estimated to be 10 months)
Treatment-induced changes in sCTX by clinical assay (Phase II only)
Baseline, cycle 1 day 1 pre-dose, cycle 1 day 8 pre-dose, cycle 1 day 15 pre-dose, day 1 of subsequent cycles (each cycle is 21 days), and end of treatment (estimated to be 10 months)
Objective response rate (ORR) (Phase II only)
Through completion of treatment (estimated to be 10 months)
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Study Design & Arms
AllocationRANDOMIZED
MaskingNONE
ModelSEQUENTIAL
PurposeTREATMENT
Treatment Arms
ArmTypeDescription
Phase Ib: Zunsemetinib + CapecitabineEXPERIMENTALPatients will receive zunsemetinib by mouth (PO) twice per day (BID) at an assigned dose along with capecitabine (1000 mg/m\^2 PO BID on Days 1-14 an every 21-day cycle). For patients enrolled in phase Ib, capecitabine is dosed on days 2-15 during cycles 1-2. Dose escalation of zunsemetinib will utilize a 3+3 design. A maximum of 3 dose levels of zunsemetinib will be tested, and the two highest dose levels which did not lead to more than 1 of 6 patients with DLT in cycle 1 will be chosen as the RP2D-L1 and RP2D-L2 for Phase II. If only one dose level of zunsemetinib was found tolerable, then only one RP2D will be chosen for Phase II.
Phase II Arm 1: Standard of care anti-resorptive + CapecitabineACTIVE_COMPARATORStandard of care anti-resorptives will consist of bisphosphonate (zoledronic acid) is to be administered every 4-12 weeks, or denosumab is to be administered every 4-6 weeks, as per physician choice and institutional practice. In general, capecitabine will be taken twice daily at a dose of 1000 mg/m\^2 on Days 1 through 14 of every 21-day cycle. The first 4 patients enrolling to phase II will take capecitabine on a different schedule for PK purposes in Cycles 1 and 2 ONLY. Patients will take capecitabine at a dose of 1000mg/m\^2 on Days 2 through 15 of Cycles 1 and 2, and then on Days 1 through 14 starting with Cycle 3.
Phase II Arm 2: Zunsemetinib (RP2D-L1) + CapecitabineEXPERIMENTALPatients will receive zunsemetinib by mouth (PO) twice per day (BID) at an assigned dose. In general, capecitabine will be taken twice daily at a dose of 1000 mg/m\^2 on Days 1 through 14 of every 21-day cycle. The first 4 patients enrolling to phase II will take capecitabine on a different schedule for PK purposes in Cycles 1 and 2 ONLY. Patients will take capecitabine at a dose of 1000mg/m\^2 on Days 2 through 15 of Cycles 1 and 2, and then on Days 1 through 14 starting with Cycle 3.
Phase II Arm 3: Zunsemetinib (RP2D-L2) + CapecitabineEXPERIMENTALPatients will receive zunsemetinib by mouth (PO) twice per day (BID) at an assigned dose. In general, capecitabine will be taken twice daily at a dose of 1000 mg/m\^2 on Days 1 through 14 of every 21-day cycle. The first 4 patients enrolling to phase II will take capecitabine on a different schedule for PK purposes in Cycles 1 and 2 ONLY. Patients will take capecitabine at a dose of 1000mg/m\^2 on Days 2 through 15 of Cycles 1 and 2, and then on Days 1 through 14 starting with Cycle 3. If only one dose level of zunsemetinib plus capecitabine was found tolerable in phase Ib testing, the phase II trial will proceed with 2:1 two-arm randomization with Arm 2 of capecitabine plus zunsemetinib and Arm 1 of capecitabine plus standard of care anti-resorptive agent.
Interventions
NameTypeDescription
ZumsemetinibDRUGPatients should take zunsemetinib at approximately the same times every day, with or without food with 8 oz of water.
CapecitabineDRUGPatients should take capecitabine at approximately the same times every day, within 30 minutes after a meal.
Zoledronic acidDRUGStandard of care. Will receive zoledronic acid or denosumab.
DenosumabDRUGStandard of care. Will receive zoledronic acid or denosumab.
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Eligibility Criteria
Age Range18 Years — N/A
SexALL
Healthy VolunteersNo
Study Sites3

Inclusion Criteria for both Phase Ib and Phase II: * Hormone receptor-positive, HER2-negative metastatic breast cancer. * Measurable or non-measurable but evaluable disease by RECIST v1.1. * Candidate for capecitabine treatment per physician decision. See below phase-specific eligibility criteria f...

Countries:United States
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Recent Changes (Last 90 Days)
LOWMay 26, 2026NCT06374459primaryCompletionDate: changed
LOWMay 24, 2026NCT06374459studyFirstPostDate: changed