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ZN-A-1041

Phase 1

Advanced Solid Tumors | Small molecule | Oncology |Roche Holding AG|Last Updated: Aug 21, 2026

Success Probability

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Market & Valuation

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Trial Design

CONTROLLED
Total Trials1
Total Enrollment210

FDA Designations

No designations recorded

Clinical trial landscape

ZN-A-1041 · 2 trials · 3 indications

Phase 1 2
NCT07051993A Study to Evaluate the Relative Bioavailability of Two Tablet Formulations Compared to Capsule Formulation and the Effect of Food and Proton Pump Inhibitor on ZN-A-1041 Tablet(s) in Healthy ParticipantsHealthy Participants
COMPLETED18 Analytics
NCT05593094A Phase 1 Trial of ZN-A-1041 Enteric Capsules or Combination in Participants With Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Advanced Solid TumorsAdvanced Solid Tumors
ACTIVE NOT_RECRUITING210 Analytics
PHASE1COMPLETED
A Study to Evaluate the Relative Bioavailability of Two Tablet Formulations Compared to Capsule Formulation and the Effect of Food and Proton Pump Inhibitor on ZN-A-1041 Tablet(s) in Healthy Participants
Healthy ParticipantsUnlock trial analytics
PHASE1ACTIVE NOT_RECRUITING
A Phase 1 Trial of ZN-A-1041 Enteric Capsules or Combination in Participants With Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Advanced Solid Tumors
Advanced Solid TumorsUnlock trial analytics

Study Endpoints

Primary Endpoints

Maximum Observed Concentration (Cmax)
Days 1-12 (Part 1)
Area Under the Concentration-Time curve from Hour 0 to the Last Measurable Concentration (AUC0-t)
Days 1-12 (Part 1)
AUC Extrapolated to Infinity (AUC0-inf)
Days 1-12 (Part 1)
Geometric Mean Ratio and Associated 90% Confidence Interval (CI) of Cmax
Days 1-12 (Part 1)
Geometric Mean Ratio and Associated 90% CI of AUC0-t
Days 1-12 (Part 1)
Geometric Mean Ratio and Associated 90% CI of AUC0-inf
Days 1-12 (Part 1)
The Incidence of Treatment-emergent Adverse Events of ZN-A-1041 as a Monotherapy in Phase 1a
23 days

Dose at which no more than one out of six participant at the same dose level experiences a probable drug-related DLT.

The Incidence of Treatment-emergent Adverse Events of ZN-A-1041 in Combination with T-DM1 or with T-DXd, or in Combination with PHESGO or Herceptin plus Perjeta
21 days

Dose at which no more than one out of six participant at the same dose level experiences a probable drug-related DLT.

RP2D
Through study completion, an average of 1 year

To evaluate the safety of ZN-A-1041 in combination with T-DM1 or with T-DXd, or in combination with PHESGO or Herceptin plus Perjeta in participants on the RP2D.

Secondary Endpoints

Time to Maximum Observed Concentration (tmax)
Days 1-12 (Part 1)
Apparent Terminal Elimination Rate Constant
Days 1-12 (Part 1)
Apparent Terminal Elimination Half-Life (t1/2)
Days 1-12 (Part 1)
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeBASIC_SCIENCE

Treatment Arms

ArmTypeDescription
Part 1: ZN-A-1041EXPERIMENTALParticipants will be administered a single dose of ZN-A-1041 orally.
1a: ZN-A-1041EXPERIMENTALPhase 1a: Participants will receive escalating doses of ZN-A-1041 orally twice a day (BID) at pre-defined dosing regimens to determine the maximum tolerated dose (MTD).
1b: ZN-A-1041 + T-DM1 3.6 mg/kg iv.EXPERIMENTALPhase 1b Arm1: 1. If the maximum tolerated dose (MTD) of ZN-A-1041 is identified in Phase 1a study: The 2 tentative dose levels of ZN-A-1041 are MTD-1 (Level 1) and MTD (Level 2). 2. If the MTD is still not reached at the maximum dose level in Phase 1a study, the maximum dose level of ZN-A-1041 in Phase 1a will be used in Phase 1b study.
1b: ZN-A-1041 + T-Dxd 5.4 mg/kg iv.EXPERIMENTALPhase 1b Arm2: 1. If the MTD of ZN-A-1041 is identified in Phase 1a study: The 2 tentative dose levels of ZN-A-1041 are MTD-1 (Level 1) and MTD (Level 2). 2. If the MTD is still not reached at the maximum dose level in Phase 1a study, the maximum dose level of ZN-A-1041 in Phase 1a will be used in Phase 1b study.
1b: ZN-A-1041 + PHESGO / Herceptin plus PerjetaEXPERIMENTALPhase 1b Arm3: 1. If the MTD of ZN-A-1041 is identified in Phase 1a study: The 2 tentative dose levels of ZN-A-1041 are MTD-1 (Level 1) and MTD (Level 2). 2. If the MTD is still not reached at the maximum dose level in Phase 1a study, the maximum dose level of ZN-A-1041 in Phase 1a will be used in Phase 1b study.
1c: ZN-A-1041 + T-DM1 3.6 mg/kg iv.EXPERIMENTALPhase 1c Arm1: The recommended dose combination for Phase 1c will be determined by the Investigator and the Sponsor based on the data from Phase 1b.
1c: ZN-A-1041 + T-Dxd 5.4 mg/kg iv.EXPERIMENTALPhase 1c Arm2: The recommended dose combination for Phase 1c will be determined by the Investigator and the Sponsor based on the data from Phase 1b.
1c: ZN-A-1041 + Herceptin plus Perjeta/PHESGOEXPERIMENTALPhase 1c Arm3: The recommended dose combination for Phase 1c will be determined by the Investigator and the Sponsor based on the data from Phase 1b.

Interventions

NameTypeDescription
ZN-A-1041DRUGParticipants will be administered either a ZN-A-1041 capsule or a tablet orally.
ZN-A-1041 + T-DM1 3.6 mg/kg iv. for Phase 1bDRUGZN-A-1041: BID via oral administration T-DM1: 3.6 mg/kg given as an intravenous infusion on the first day of each treatment cycle, once every 3 weeks (21-day cycle)
ZN-A-1041 + T-Dxd 5.4 mg/kg iv. for Phase 1bDRUGZN-A-1041: BID via oral administration T-DXd: 5.4 mg/kg given as an intravenous infusion on the first day of each treatment cycle, once every 3 weeks (21-day cycle)
ZN-A-1041 + PHESGO / Herceptin plus Perjeta injection for Phase 1bDRUGZN-A-1041: BID via oral administration PHESGO dose is 600 mg pertuzumab/600 mg trastuzumab/2000 unites hyaluronidase every 3 weeks for subcutaneous administrations (21-day cycle) Perjeta is 420 mg administered as an intravenous infusion Herceptin is 6 mg/kg administered as an intravenous infusion
ZN-A-1041 + T-DM1 3.6 mg/kg iv. for Phase 1cDRUGZN-A-1041: BID via oral administration T-DM1: intravenous infusion on the first day of each treatment cycle, once every 3 weeks (21-day cycle)
ZN-A-1041 + T-Dxd 5.4 mg/kg iv. for Phase 1cDRUGZN-A-1041: BID via oral administration T-DXd: intravenous infusion on the first day of each treatment cycle, once every 3 weeks (21-day cycle)
ZN-A-1041 + PHESGO / Herceptin plus Perjeta injection for Phase 1cDRUGZN-A-1041: BID via oral administration PHESGO: every 3 weeks for subcutaneous administrations (21-day cycle) Perjeta: intravenous infusion Herceptin: intravenous infusion
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Eligibility Criteria

Age Range18 Years to 75 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Body mass index (BMI) within the range of 18 to 32 kg/m\^2, inclusive * Negative hepatitis panel and negative HIV antibody screens * Negative screening test for latent Mycobacterium tuberculosis infection * Able to consume the high-fat meal within the protocol-specified time p...

Countries:United KingdomUnited StatesAustraliaFranceItalyNew ZealandSpain
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Competitive Landscape -Other Solid Tumors 9 trials (matched to "Advanced Solid Tumors")

Recent Changes (Last 90 Days)

LOWAug 21, 2026NCT05593094lastUpdatePostDate: changed
LOWAug 21, 2026NCT05593094lastUpdatePostDate: changed

Frequently asked questions about ZN-A-1041

What is ZN-A-1041 used for?

ZN-A-1041 is an investigational small molecule being studied for the treatment of HER2-positive advanced solid tumors, including HER2-positive breast cancer. It is also being evaluated in healthy participants to assess the bioavailability of different tablet formulations compared to the capsule formulation, and the effect of food and proton pump inhibitors on the drug.

Who makes ZN-A-1041?

ZN-A-1041 is being developed by Roche Holding AG, which trades under the ticker RHHBY. The company is conducting clinical trials to evaluate the drug in patients with HER2-positive advanced solid tumors and in healthy participants for formulation studies.

What phase is ZN-A-1041 in?

ZN-A-1041 is in Phase 1 clinical development. It is an investigational drug and has not been approved by regulatory authorities. The ongoing Phase 1 trial is active but not recruiting participants, and a separate Phase 1 study in healthy participants has been completed.

What clinical trials is ZN-A-1041 in?

ZN-A-1041 is being studied in two Phase 1 clinical trials. The first, NCT05593094, is an active trial in participants with HER2-positive advanced solid tumors, enrolling 210 participants across the United States, Australia, France, Italy, New Zealand, Spain, and the United Kingdom. The second, NCT07051993, is a completed study in healthy participants in the United Kingdom.

What does ZN-A-1041 target?

ZN-A-1041 targets the human epidermal growth factor receptor 2 (HER2). It is being studied in patients with HER2-positive advanced solid tumors, including HER2-positive breast cancer, as a single agent or in combination with other therapies.