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A Study to Test Different Doses of BI 3011441 in Japanese People With Different Types of Advanced Cancer (NRAS/KRAS Mutation Positive)

Phase 1
Completed
Conditions
Solid Tumors, KRAS Mutation
Interventions
Registration Number
NCT04742556
Lead Sponsor
Boehringer Ingelheim
Brief Summary

This study is open to Japanese adults with different types of advanced cancer that are positive for NRAS/KRAS mutations. This is a study in people for whom previous treatment was not successful or no standard treatment exists.

The purpose of this study is to find the highest dose of BI 3011441 that Japanese people with advanced cancer can tolerate. BI 3011441 is a medicine that may turn off a signal by NRAS/KRAS that makes tumours grow.

Participants take BI 3011441 as capsules once a day. Participants can stay in the study as long as they benefit from treatment and can tolerate it. The doctors collect information on any health problems of the participants.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
15
Inclusion Criteria
  • Must be at least 20 years of age at screening.
  • Signed and dated written informed consent in accordance with Good Clinical Practice(GCP) and local legislation prior to admission to the trial.
  • Pathologically documented, locally-advanced or metastatic malignancy with previously identified activating Neuroblastoma RAS viral (v-ras) oncogene homolog (NRAS) or Kirsten rat sarcoma viral oncogene homologue (KRAS) mutation based on local test.
  • Provision of archival tumor tissue, if available, to confirm retrospectively NRAS or KRAS mutation status and for biomarker assessment.
  • Willingness to undergo pre- and on-treatment tumour biopsies for pharmacodynamics and biomarker assessment. Patients can be enrolled without tumour biopsy upon agreement between the Investigator and the Sponsor if tumour biopsy is not feasible (Apply only to study site which agreed to conduct biopsy).
  • Must have either progressed despite appropriate prior standard therapies or for whom no standard therapy exists for their tumour type and disease stage
  • Must have at least one target lesion that can be measured per Response Evaluation Criteria in Solid Tumours (RECIST) version 1.1
  • Must have an Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1.

Further inclusion criteria apply.

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

  • Radiotherapy within 4 weeks prior to first administration of BI 3011441 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 within 4 weeks prior to start of treatment or scheduled during the projected course of the trial

  • Previous treatment with a Rat sarcoma (RAS), Mitogen-activated protein kinase (MAPK) targeting agent

  • Previous treatment with any investigational agent(s) or targeted treatment within 4 weeks (28 days) prior to start of trial drug or concurrent participation in another clinical trial with an investigational device or drug.

  • Any history of or concomitant condition that, in the opinion of the investigator, would compromise the patient's ability to comply with the study or interfere with the evaluation of the efficacy and safety of the study medications

  • Patients who have a history or current evidence/risk of retinal vein occlusion (RVO) or retinal pigment epithelial detachment or central serous retinopathy; for example, predisposing factors of RVO or central serous retinopathy include uncontrolled glaucoma or ocular hypertension, history of hyperviscosity or hypercoagulability syndromes.

  • Patients who have visible retinal pathology that is considered a risk factor for RVO or central serous retinopathy as assessed by ophthalmic examination, such as:

    • Evidence of new optic disc cupping
    • Evidence of new visual field defects
    • Intraocular pressure >21 mm Hg History or presence of cardiovascular abnormalities such as uncontrolled hypertension, congestive heart failure New York Heart Association (NYHA) classification of ≥2, unstable angina or poorly controlled arrhythmia which are considered as 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.

Further exclusion criteria apply.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
8 mg BI 3011441BI 3011441The patients were administered 8 milligram (mg) BI 3011441 soft capsule once daily during 4 weeks with water limited to a maximum of 100 milliliters (mL) per capsules, taken without food, at least 1 hour before a meal or 1 hour after a meal. Patients continued the treatment until undue drug toxicity, disease progression, or withdrawal of consent, whichever occurred first.
4 mg BI 3011441BI 3011441The patients were administered 4 milligram (mg) BI 3011441 soft capsule once daily during 4 weeks with water limited to a maximum of 100 milliliters (mL) per capsules, taken without food, at least 1 hour before a meal or 1 hour after a meal. Patients continued the treatment until undue drug toxicity, disease progression, or withdrawal of consent, whichever occurred first.
6 mg BI 3011441BI 3011441The patients were administered 6 milligram (mg) BI 3011441 soft capsule once daily during 4 weeks with water limited to a maximum of 100 milliliters (mL) per capsules, taken without food, at least 1 hour before a meal or 1 hour after a meal. Patients continued the treatment until undue drug toxicity, disease progression, or withdrawal of consent, whichever occurred first.
Primary Outcome Measures
NameTimeMethod
Number of Patients With DLTs in the MTD Evaluation PeriodFirst treatment cycle, the first 28 days following the start of trial medication.

Number of participants with Dose limiting toxicities (DLT) occurring during the first treatment cycle (first 4 weeks). DLT was defined as any of the following adverse events related to the treatment:

* Haematologic toxicities:

* Neutropenia Grade 4 lasting for \>7 days days without documented infection

* Neutropenia Grade ≥3 with documented infection

* Grade ≥3 febrile neutropenia

* Grade 4 neutropenia defined as life-threatening consequences or urgent intervention indicated

* Grade 5 neutropenia defined as a fatal neutropenia

* Grade 3 thrombocytopenia associated with bleeding

Maximum Tolerated Dose (MTD) of BI 3011441 MonotherapyFirst treatment cycle, the first 28 days following the start of trial medication.

Maximum tolerated dose (MTD) of BI 3011441 monotherapy. The MTD was defined as the highest dose with less than 25% risk of the true dose-limiting toxicity (DLT) rate being equal or above 0.33 (EWOC criterion) during the MTD evaluation period. The analysis of the MTD was based on a Bayesian 2-parameter logistic regression model (BLRM) with overdose control.

Secondary Outcome Measures
NameTimeMethod
Number of Patients With DLTs During the Entire On-treatment PeriodFrom first BI 3011441 intake until last BI 3011441 intake + 30 days of Residual effect period (REP), up to 373 days.

Number of participants with Dose limiting toxicities (DLT) occurring during the first treatment cycle (first 4 weeks). DLT was defined as any of the following adverse events related to the treatment:

* Haematologic toxicities:

* Neutropenia Grade 4 lasting for \>7 days days without documented infection

* Neutropenia Grade ≥3 with documented infection

* Grade ≥3 febrile neutropenia

* Grade 4 neutropenia defined as life-threatening consequences or urgent intervention indicated

* Grade 5 neutropenia defined as a fatal neutropenia

* Grade 3 thrombocytopenia associated with bleeding

Number of Patients With Grade ≥3 Treatment-related Adverse EventsFrom first BI 3011441 intake until last BI 3011441 intake + 30 days of Residual effect period (REP), up to 373 days.

Number of participants with Grade ≥3 treatment-related adverse events is reported. The severity of AEs were assessed according to the Common Terminology Criteria for Adverse Events (CTCAE) Version 5.0. The CTCAE grades are Grade 3 (severe AE), 4 (life-threatening or disabling AE), 5 (death related to AE).

Number of Patients With Treatment Related Adverse EventsFrom first BI 3011441 intake until last BI 3011441 intake + 30 days of Residual effect period (REP), up to 373 days.

Number of participants with drug-related adverse events (AEs) analysed as investigator defined drug-related AEs is presented. Medical judgment was used to determine the relationship between the AEs and the study medication, considering all relevant factors, including pattern of reaction, temporal relationship, de-challenge or re-challenge, confounding factors such as concomitant medication, concomitant diseases and relevant history.

Area Under the Concentration-time Curve of BI 3011441 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)Cycle 1: Day 1: Within 5 minutes (min) before and 30min, 45min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h and optionally 12h. and Day 2 : Within 5 minutes (min) before dosing on Day 2.

Area under the concentration-time curve of BI 3011441 in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) is reported.

Area Under the Concentration-time Curve of BI 3011441 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point at Steady State (AUC0-tz,ss)Cycle 1: Day 15: Within 5 minutes (min) before drug administration on Day 15, and 30min, 45min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h and optionally 12h. and Day 16 : Within 5 minutes (min) before dosing on Day 16.

Area under the concentration-time curve of BI 3011441 in plasma over the time interval from 0 to the last quantifiable data point at steady state (AUC0-tz,ss) is reported.

Maximum Measured Concentration of BI 3011441 in Plasma After First Dose (Cmax)Cycle 1: Day 1: Within 5 minutes (min) before and 30min, 45min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h and optionally 12h. and Day 2 : Within 5 minutes (min) before dosing on Day 2.

Maximum measured concentration of BI 3011441 in plasma (Cmax) is reported.

Maximum Measured Concentration of BI 3011441 in Plasma at Steady State (Cmax,ss)Cycle 1: Day 15: Within 5 minutes (min) before drug administration on Day 15, and 30min, 45min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h and optionally 12h. and Day 16 : Within 5 minutes (min) before dosing on Day 16.

Maximum measured concentration of BI 3011441 in plasma at steady state (Cmax,ss) is reported. PK samples were collected at the following timepoints.

Trial Locations

Locations (3)

National Cancer Center Hospital

🇯🇵

Tokyo, Chuo-ku, Japan

Japanese Foundation for Cancer Research

🇯🇵

Tokyo, Koto-ku, Japan

National Cancer Center Hospital East

🇯🇵

Chiba, Kashiwa, Japan

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