MedPath

A Study to Find a Safe and Effective Dose of BI 1701963 Alone and in Combination With BI 3011441 in Patients With Advanced Cancer and a Certain Mutation (Kirsten Rat Sarcoma Viral Oncogene Homologue [KRAS])

Phase 1
Terminated
Conditions
Solid Tumors, KRAS Mutation
Interventions
Registration Number
NCT04835714
Lead Sponsor
Boehringer Ingelheim
Brief Summary

This is a study in adults with advanced cancer (solid tumours including non-small cell lung cancer and colorectal cancer) in whom previous chemotherapy was not successful. People who have a tumour with a KRAS mutation can participate in the study. A KRAS mutation makes cancer grow faster.

The study tests 2 medicines called BI 1701963 and BI 3011441. BI 1701963 and BI 3011441 prevent activation of KRAS.

The purpose of this study is to find out the highest dose of BI 1701963 alone and in combination with BI 3011441 the participants can tolerate. Another purpose is to check whether BI 1701963 in combination with BI 3011441 is able to make tumours shrink.

Participants can stay in the study as long as they benefit from treatment and can tolerate it. During this time, they get tablets of BI 1701963 and capsules of BI 3011441 once daily. The doctors regularly monitor the size of the tumour. Doctors also regularly record any unwanted effects and check participants' health.

Detailed Description

Not available

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
8
Inclusion Criteria
  • Previously-identified activating Kirsten rat sarcoma viral oncogene homologue (KRAS) mutation in tumour tissue or blood prior to screening. Activating mutations may include but are not limited to: KRAS mutations in expressed region (exon) 2 (G12, G13), exon 3 (A59, Q61) and exon 4 (K117, A146).

  • Provision of archival tumour tissue, if available, to confirm retrospectively KRAS mutation status and for biomarker assessment

  • At least one target lesion that can be measured per Response Evaluation Criteria In Solid Tumours (RECIST) version 1.1. In patients who only have one target lesion, and a biopsy of the lesion is required, the baseline imaging must be performed at the earliest two weeks after the biopsy.

  • Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1 at screening

  • Adequate organ function at screening as follows:

    • Absolute neutrophil count (ANC) ≥1.5 x 109/L; hemoglobin ≥9.0 g/dL; platelets ≥100 x 109/L without the use of haematopoietic growth factors or recent transfusion
    • Total bilirubin ≤1.5 times the upper limit of normal (ULN), or ≤4 x ULN for patients who are known to have Gilbert's syndrome.
    • Creatinine ≤1.5 x ULN. If creatinine is >1.5 x ULN, patient is eligible if concurrent glomerular filtration rate (GFR) ≥50 mL/min (measured or calculated by Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) formula).
    • Aspartate transaminase (AST) and alanine transaminase (ALT) ≤3 x ULN if no demonstrable liver metastases, or ≤ 5 x ULN if transaminase elevation is attributable to liver metastases.
  • Age ≥18 years of age, or over the legal age of consent as required by local legislation at informed consent.

  • Recovery from any previous therapy related toxicity to Common Terminology Criteria for Adverse Events (CTCAE) Grade ≤1 at Cycle 1 Day 1 (except for alopecia, stable sensory neuropathy must be CTCAE Grade ≤2 and except for amenorrhea/menstruation related disorders of any grade) before the first dose.

  • Signed and dated written informed consent in accordance with Good Clinical Practice (GCP) and local legislation prior to admission to the trial.

Further inclusion criteria apply.

Exclusion Criteria
  • Previous anticancer chemotherapy or anticancer immunotherapy within 3 weeks of the first administration of trial drug. Previous anticancer hormonal treatment within 2 weeks of the first administration of trial drugs.

  • Previous treatment with Rat sarcoma (RAS), Mitogen-activated protein kinase (MAPK) or Son of Sevenless 1 (SOS1) targeting agents

  • Radiotherapy within 4 weeks prior to start of treatment except as follows

    • Palliative radiotherapy to regions other than the chest is allowed up to 2 weeks prior to start of treatment
    • Single dose palliative radiotherapy for symptomatic metastasis within 2 weeks prior to start of treatment may be allowed but must be discussed with the sponsor.
  • Major surgery (major according to the investigator's assessment) performed within 4 weeks prior to start of treatment or planned during the projected course of the trial, e.g. hip replacement.

  • Previous treatment with any investigational agent(s) or targeted treatment within 28 days prior to start of treatment.

  • Known history of hypersensitivity to any of the excipients of BI 1701963 tablets

  • History or presence of cardiovascular abnormalities such as uncontrolled hypertension, congestive heart failure New-York-Heart-Assocation (NYHA) classification of ≥3, unstable angina or poorly controlled arrhythmia which are considered clinically relevant by the investigator; myocardial infarction within 6 months prior to start of treatment. Uncontrolled hypertension is defined as: Blood pressure (BP) measured in a rested and relaxed condition, where systolic BP ≥140 mmHg, or diastolic BP ≥90 mmHg, with or without medication.

  • Left ventricular ejection fraction (LVEF) <50 %. Further exclusion criteria apply.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Part C with Combination therapy dose confirmationBI 3011441-
Part D with Combination therapy dose expansionBI 1701963-
Part B with Combination therapy dose escalationBI 3011441-
Part C with Combination therapy dose confirmationBI 1701963-
Part D with Combination therapy dose expansionBI 3011441-
Part A with Monotherapy dose escalationBI 1701963-
Part B with Combination therapy dose escalationBI 1701963-
Primary Outcome Measures
NameTimeMethod
Number of patients with dose-limiting toxicities (DLTs) in the Maximum tolerated dose (MTD) evaluation period in monotherapy (Part A)Up to 28 days
Objective response (OR) defined as best overall response of confirmed complete response (CR) or confirmed partial response (PR) in combination therapy dose confirmation (Part C)Up to 12 months

Best overall response is defined according to Response Evaluation Criteria In Solid Tumours (RECIST) version 1.1 as assessed by the investigator and will consider all tumour assessments from first administration until disease progression or death (whichever occurs first) or last evaluable tumour assessment before start of subsequent anticancer therapy, loss to follow-up or withdrawal of consent.

Number of patients with dose-limiting toxicities (DLTs) in the Maximum tolerated dose (MTD) evaluation period in combination therapy (Part B)Up to 28 days
Objective response (OR) defined as best overall response of confirmed complete response (CR) or confirmed partial response (PR) in combination therapy dose expansion (Part D)Up to 12 months

Best overall response is defined according to Response Evaluation Criteria In Solid Tumours (RECIST) version 1.1 as assessed by the investigator and will consider all tumour assessments from first administration until disease progression or death (whichever occurs first) or last evaluable tumour assessment before start of subsequent anticancer therapy, loss to follow-up or withdrawal of consent.

Secondary Outcome Measures
NameTimeMethod
Area under the plasma concentration-time curve over the time interval from 0 to the last quantifiable data point (AUC0-tz) of BI 1701963 after the first dose in monotherapy (Part A)Up to 24 hours
Maximum plasma concentration at steady state (Cmax,ss) of BI 1701963 after multiple doses in monotherapy (Part A)Up to 12 weeks
Maximum plasma concentration at steady state (Cmax,ss) of BI 3011441 after multiple doses (Part B only)Up to 12 weeks
Number of patients with Common Terminology Criteria for Adverse Events (CTCAE) Grade ≥3 treatment-related adverse events observed during the on-treatment period in combination therapy dose confirmation (Part C)Up to 12 months
Maximum plasma concentration at steady state (Cmax,ss) of BI 1701963 after multiple doses in combination therapy dose expansion (Part D)Up to 12 weeks
Maximum plasma concentration (Cmax) of BI 3011441 after the first dose in combination therapy dose expansion (Part D)Up to 24 hours
Maximum plasma concentration (Cmax) of BI 1701963 after the first dose in combination therapy (Part B)Up to 24 hours
Area under the concentration-time curve at steady state over the uniform dosing interval τ (AUCτ,ss) of BI 3011441 after multiple doses (Part B only)Up to 12 weeks
Maximum plasma concentration (Cmax) of BI 1701963 after the first dose in monotherapy (Part A)Up to 24 hours
Area under the plasma concentration-time curve over the time interval from 0 to the last quantifiable data point (AUC0-tz) of BI 1701963 after the first dose in combination therapy (Part B)Up to 24 hours
Maximum plasma concentration at steady state (Cmax,ss) of BI 1701963 after multiple doses in combination therapy (Part B)Up to 12 weeks
Area under the concentration-time curve at steady state over the uniform dosing interval τ (AUCτ,ss) of BI 1701963 after multiple doses in monotherapy (Part A)Up to 12 weeks
Area under the concentration-time curve at steady state over the uniform dosing interval τ (AUCτ,ss) of BI 1701963 after multiple doses in combination therapy (Part B)Up to 12 weeks
Maximum plasma concentration (Cmax) of BI 3011441 after the first dose (Part B only)Up to 24 hours
Area under the plasma concentration-time curve over the time interval from 0 to the last quantifiable data point (AUC0-tz) of BI 3011441 after the first dose (Part B only)Up to 24 hours
Number of patients with Common Terminology Criteria for Adverse Events (CTCAE) Grade ≥3 treatment-related adverse events observed during the on-treatment period in combination therapy dose expansion (Part D)Up to 12 months
Area under the concentration-time curve at steady state over the uniform dosing interval τ (AUCτ,ss) of BI 3011441 after multiple doses in combination therapy dose confirmation (Part C)Up to 12 weeks
Area under the concentration-time curve at steady state over the uniform dosing interval τ (AUCτ,ss) of BI 3011441 after multiple doses in combination therapy dose expansion (Part D)Up to 12 weeks
Tumour shrinkage (in millimetres) in combination therapy dose confirmation (Part C)Up to 12 months

Tumour shrinkage (in millimetres) is defined as the difference between the minimum post-baseline sum of diameters of target lesions (longest for non-nodal lesions, short axis for nodal lesions) and the baseline sum of longest diameters of the same set of target lesions.

Progression-free survival (PFS) rate at 6 months in combination therapy dose confirmation (Part C)Up to 6 months

Based on PFS defined as the time from first administration until tumour progression according to RECIST 1.1 or death from any cause, whichever occurs earlier

Maximum plasma concentration (Cmax) of BI 1701963 after the first dose in combination therapy dose confirmation (Part C)Up to 24 hours
Maximum plasma concentration (Cmax) of BI 1701963 after the first dose in combination therapy dose expansion (Part D)Up to 24 hours
Area under the plasma concentration-time curve over the time interval from 0 to the last quantifiable data point (AUC0-tz) of BI 1701963 after the first dose in combination therapy dose confirmation (Part C)Up to 24 hours
Area under the concentration-time curve at steady state over the uniform dosing interval τ (AUCτ,ss) of BI 1701963 after multiple doses in combination therapy dose confirmation (Part C)Up to 12 weeks
Maximum plasma concentration (Cmax) of BI 3011441 after the first dose in combination therapy dose confirmation (Part C)Up to 24 hours
Area under the plasma concentration-time curve over the time interval from 0 to the last quantifiable data point (AUC0-tz) of BI 3011441 after the first dose in combination therapy dose confirmation (Part C)Up to 24 hours
Area under the plasma concentration-time curve over the time interval from 0 to the last quantifiable data point (AUC0-tz) of BI 3011441 after the first dose in combination therapy dose expansion (Part D)Up to 24 hours
Maximum plasma concentration at steady state (Cmax,ss) of BI 3011441 after multiple doses in combination therapy dose confirmation (Part C)Up to 12 weeks
Maximum plasma concentration at steady state (Cmax,ss) of BI 3011441 after multiple doses in combination therapy dose expansion (Part D)Up to 12 weeks
Duration of Objective Response (OR) in combination therapy dose expansion (Part D)Up to 12 months

Duration of OR is defined as the time from first documented CR or PR until disease progression or death (whichever occurs first) among patients with OR.

Area under the plasma concentration-time curve over the time interval from 0 to the last quantifiable data point (AUC0-tz) of BI 1701963 after the first dose in combination therapy dose expansion (Part D)Up to 24 hours
Maximum plasma concentration at steady state (Cmax,ss) of BI 1701963 after multiple doses in combination therapy dose confirmation (Part C)Up to 12 weeks
Area under the concentration-time curve at steady state over the uniform dosing interval τ (AUCτ,ss) of BI 1701963 after multiple doses in combination therapy dose expansion (Part D)Up to 12 weeks
Duration of Objective Response (OR) in combination therapy dose confirmation (Part C)Up to 12 months

Duration of OR is defined as the time from first documented CR or PR until disease progression or death (whichever occurs first) among patients with OR.

Tumour shrinkage (in millimetres) in combination therapy dose expansion (Part D)Up to 12 months

Tumour shrinkage (in millimetres) is defined as the difference between the minimum post-baseline sum of diameters of target lesions (longest for non-nodal lesions, short axis for nodal lesions) and the baseline sum of longest diameters of the same set of target lesions.

Progression-free survival (PFS) rate at 6 months in combination therapy dose expansion (Part D)Up to 6 months

Based on PFS defined as the time from first administration until tumour progression according to RECIST 1.1 or death from any cause, whichever occurs earlier

Trial Locations

Locations (4)

National Cancer Center Hospital East

🇯🇵

Chiba, Kashiwa, Japan

National Cancer Center Hospital

🇯🇵

Tokyo, Chuo-ku, Japan

Aichi Cancer Center Hospital

🇯🇵

Aichi, Nagoya, Japan

Japanese Foundation for Cancer Research

🇯🇵

Tokyo, Koto-ku, Japan

© Copyright 2025. All Rights Reserved by MedPath