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No longer recruiting (closed or complete)Last updated: 14 March 2025

This Phase I trial is trying to determine how safe and tolerable a targeted therapy (BGB-3245) is in people with solid cancers with B-RAF genetic mutations.A First-in-Human, Phase 1a/1b, Open Label, Dose-Escalation and Expansion Study to Investigate the Safety, Pharmacokinetics, and Antitumor Activity of the RAF Dimer Inhibitor BGB-3245 in Patients With Advanced or Refractory Tumors

Trial purpose

Medical clipboardCancer treatment

Tumor type

Multi-Cancer Multi-Cancer

Age

People18+

Clinical summary

Summary

This is a non-randomised dose escalation and dose expansion study assessing BGB-3245 in people with tumours harbouring B-RAF mutations that are likely to respond to a RAF dimer inhibitor. Phase 1a will consist of a dose-escalation and dose finding component to establish the MTD and/or RP2D in participants with MAPK pathway aberrations. In this, phase participants will receive BGB-3245 (orally) as a continuous daily administration, in 28 day and 30 day cycles. Phase 1b will consist of a dose expansion component and is split into two groups. Phase 1b, Group 1 is focusing on dose expansion in non-V600 B-RAF mutations. BGB3245 will be administered (orally) as a continuous daily administration, in 28 day and 30 day cycles in participants with non-V600 B-RAF including RAF fusions. Phase 1b, Group 2, is focus on dose expansion in B-RAF V600 mutations. BGB-3245 will be administered (orally) as a continuous daily administration, in 28 day and 30 day cycles in participants with B-RAF V600mutatted melanoma or NSCLC B-RAF and/or MEK inhibitor resistant tumours (i.e. have progressed on a B-RAF-inhibitor and/or MEK-inhibitor).

Conditions

This trial is treating people with solid cancers with B-RAF genetic mutations

Eligibility

Inclusion

  1. Participants with histologically confirmed advanced or metastatic solid tumor who had disease progression during or after systemic anticancer therapies that previously demonstrated clinical benefit (eg, improved survival) in a representative population, or are unable to receive standard therapy(ies). In addition, participants must meet the following eligibility criteria for the corresponding phase of the study:

    1. Phase 1a: participants with a known mutation status and tumor harboring an oncogenic mutation of the v-RAF murine sarcoma viral oncogene homolog B (BRAF) gene (the mutations of primary interest are the BRAF Class II mutation, Class III mutation or BRAF fusion). In addition, participants with tumors harboring the mutation of the neuroblastoma RAS viral oncogene homolog (NRAS) gene or the Kirsten rat sarcoma virus oncogene homolog (KRAS) are eligible for Part 1a. For participants with KRAS mutations, tumor types of colorectal cancer (CRC) and pancreatic cancer are excluded.
    2. Phase 1b: participants must have a known mutation status and meet one of the following criteria according to the group they are enrolled into:

    I. Group 1: participants with tumor types other than CRC that harbor BRAF V600 mutations who have been treated and progressed on prior BRAF and/or mitogen activated protein kinase (MEK) inhibition.

    a. Participants must have received the last dose of prior BRAF and/or MEK inhibitor therapy within 90 days of initiation of BGB-3245 study treatment (Cycle 1 Day 1)

    II. Group 2: participants with advanced solid tumors harboring a BRAF Class II mutation or a BRAF fusion mutation.

  2. Participants must provide archival tumor tissue or agree to a fresh tumor biopsy for mutation and biomarkers analysis (fresh tumor biopsies are strongly recommended)
  3. Participants must have radiologically measurable disease as defined by RECIST v1.1
  4. Eastern Cooperative Oncology Group (ECOG) performance status of ≤1
  5. Adequate organ function and no transfusions within 14 days of first dose

Exclusion

  1. Participants receiving cancer therapy (chemotherapy or other systemic anticancer therapies, immunotherapy, radiation therapy, or surgery) at the time of Cycle 1 Day 1.
  2. All participants who have received prior systemic anticancer treatment within the following time frames will be excluded:

    1. Systemic chemotherapy within 4 weeks or 6 weeks for nitrosourea, mitomycin prior to Cycle 1 Day 1; and
    2. Biologic therapy (i.e., antibodies), continuous or intermittent small-molecule therapies, or any other investigational agents within a period of 5 times the half-life of the agent or ≤4 weeks (whichever is shorter) prior to Cycle 1 Day 1.
  3. Severe or uncontrolled systemic disease.
  4. Clinically significant cardiac disease within 6 months of signing the ICF
  5. CNS metastases, leptomeningeal carcinomatosis or untreated spinal cord compression.
  6. Inability to swallow oral medicines.
  7. Any unstable, preexisting major medical condition, including known human immunodeficiency virus (HIV) or active hepatitis B virus (HBV) or hepatitis C virus (HCV) infection.
  8. Systemic anti-cancer therapy within 2 weeks or 5 half-lives before first dose.
  9. Major surgical procedure or significant traumatic injury within 4 weeks prior to the first dose or anticipates need for major surgery while on study.

NOTE: Other protocol defined Inclusion/Exclusion criteria may apply.

Inclusion

  • Your cancer has not spread to other parts of the body (localised).
  • You have had treatment but your cancer has gotten worse or has not responded to the treatment you have been given.
  • You are able to swallow medication by mouth.

Exclusion

  • You have certain types of non-cancer medical conditions.
  • You have had certain treatments, surgical procedures or drugs.
Message

Clinical trials have complex eligibility criteria, and other criteria may apply for this trial. Ask your doctor about whether this trial could be right for you.

Participating hospitals

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No longer recruiting (closed or complete) hospitals

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More information

Trial Identifiers

Information on this page is partially produced from ClinicalTrials.gov *. View further details about this trial on the registry via the links below:

Trial sponsor

MapKure, LLC

Scientific Title

A First-in-Human, Phase 1a/1b, Open Label, Dose-Escalation and Expansion Study to Investigate the Safety, Pharmacokinetics, and Antitumor Activity of the RAF Dimer Inhibitor BGB-3245 in Patients With Advanced or Refractory Tumors

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