XP-102 and XP-102 in Combination With Trametinib in Advanced Solid Tumor Patients With a BRAF V600 Mutation

NCT05275374 | Not Yet Recruiting Phase 1 FDA Drug

• 1 other identifier: XYN-701
• Study Type: interventional
• Target: 221
• Locations: 0 countries
• Sites: N/A

Brief Summary

This is a first-in-human multi-center study which will be conducted in advanced malignant solid tumors patients. The solid tumor type is limited to melanoma, colorectal, non-small-cell lung, and thyroid cancer with positive BRAF V600 mutation. This study is divided into three stages: Phase Ia: a dose-escalation phase of XP-102; Phase Ib: a dose-escalation and sample size expansion phase of XP-102 plus trametinib; Phase IIa: an expansion phase of XP-102 plus trametinib.

Conditions

Cancer; BRAF V600 Mutation; Melanoma; Colorectal Cancer; Thyroid Cancer; Nonsmall Cell Lung Cancer

Outcome Measures

Primary Outcomes (3)

• Characterize the safety of XP-102.

  Number of participants with treatment related adverse events.

  28 days

• Evaluate the pharmacokinetics of XP-102.

  Blood plasma concentration.

  28 days

• Establish maximum tolerated dose of XP-102.

  Number of participants with dose limiting toxicity

  28 days

Secondary Outcomes (4)

• Evaluate the pharmacokinetics of XP-102 + trametinib.

  28 days

• Characterize tolerability of XP-102 in combination with trametinib.

  28 days

• Evaluate the pharmacokinetics of XP-102 administered with food

  4 days

• Evaluate clinical activity/efficacy of XP-102.

  Approximately every 8 weeks (up to 2 years)

Study Arms (3)

Part 1 - XP-102 Dose Escalation

EXPERIMENTAL

XP-102

Drug: XP-102

Part 2 - XP-102 + Trametinib Dose Escalation

EXPERIMENTAL

XP-102 plus Trametinib

Drug: XP-102; Drug: Trametinib

Part 3 - XP-102 + Trametinib Dose Expansion

EXPERIMENTAL

XP-102 plus Trametinib

Drug: XP-102; Drug: Trametinib

Interventions

XP-102 DRUG

XP-102 will be administered orally once or twice daily in a continuous regimen.

Part 1 - XP-102 Dose Escalation; Part 2 - XP-102 + Trametinib Dose Escalation; Part 3 - XP-102 + Trametinib Dose Expansion

Trametinib DRUG

Trametinib will be administered 2mg orally once a day.

Part 2 - XP-102 + Trametinib Dose Escalation; Part 3 - XP-102 + Trametinib Dose Expansion

Eligibility Criteria

• Age: 18 Years+
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• ≥18 years of age
• Advanced malignant solid tumor patients with a BRAF V600 mutation (limited to melanoma, colorectal cancer, non-small cell lung cancer, or thyroid cancer).
• Must have failed conventional treatment or for whom no therapy of proven efficacy exists or who is not eligible for established treatment options. Prior treatment with BRAF inhibitors and/or MEK inhibitors is permitted；
• At least one measurable lesion (brain metastasis must not be the only measurable lesion) according to Response Evaluation Criteria in Solid Tumours (RECIST v1.1);
• ECOG performance status of 0 or 1;
• Expected survival ≥ 3 months;
• Adequate liver, renal, coagulation, cardiac, and hematologic function.
• A negative pregnancy test if female patient is of reproductive potential.
• For men and women of reproductive potential, agreement to use an effective contraceptive method from the time of screening and throughout their time on study.
• Patients must agree to, and be capable of, adhering to the study visit schedule and all other protocol requirements;
• Patients must understand and voluntarily sign the written informed consent form, before the initiation of any study-specific procedures in the trial.

You may not qualify if:

• Active central nervous system (CNS) lesions. However, patients with asymptomatic and brain metastases who received treatment (including targeted brain radiotherapy, surgical treatment, glucocorticoid or other treatments) without disease progression for ≥ 3 months are eligible.
• Patients who received radiotherapy, immunotherapy, hormone therapy, targeted therapy, biotherapy, traditional Chinese medicine therapy, chemotherapy or any clinical trial treatment within 14 days before the first dose.
• Patients who have persistent toxicity caused by previous chemotherapeutic drugs or radiotherapy has not recovered to lower than grade 2 (except hair loss) according to CTCAE version 5.0;
• Patients who are allergic to active substances or excipients of XP-102 or trametinib.
• Significant traumatic injury within 28 days before the first dose of the investigational drug, or if major surgery is anticipated during the course of study treatment;
• According to the judgment of the investigator, patients with dysphagia, or any gastrointestinal diseases that may affect drug absorption or activity;
• Administration of strong inhibitors or inducers of CYP3A4 liver metabolic enzymes within 14 days before the first dose of the investigational drug;
• Patients who are receiving drugs that may prolong QT interval and unable or unwilling to stop treatment or switch to other alternative treatment before study enrollment;
• Symptomatic active fungal, bacterial and/or viral infections; including known HIV, active hepatitis B, active hepatitis C or active syphilis infection.
• Any poorly controlled disorders (such as serious mental, neurological, cardiovascular, respiratory, digestive, urinary, bleeding and coagulation, or other system diseases) that may significantly affect the clinical trial;
• Other situations not suitable for participation in the study as judged by the investigator.

Sponsors & Collaborators

• Xynomic Pharmaceuticals, Inc.: lead

MeSH Terms

Conditions

Neoplasms; Melanoma; Colorectal Neoplasms; Thyroid Neoplasms; Carcinoma, Non-Small-Cell Lung

Interventions

trametinib

Condition Hierarchy (Ancestors)

Neuroendocrine Tumors; Neuroectodermal Tumors; Neoplasms, Germ Cell and Embryonal; Neoplasms by Histologic Type; Neoplasms, Nerve Tissue; Nevi and Melanomas; Skin Neoplasms; Neoplasms by Site; Skin Diseases; Skin and Connective Tissue Diseases; Intestinal Neoplasms; Gastrointestinal Neoplasms; Digestive System Neoplasms; Digestive System Diseases; Gastrointestinal Diseases; Colonic Diseases; Intestinal Diseases; Rectal Diseases; Endocrine Gland Neoplasms; Head and Neck Neoplasms; Endocrine System Diseases; Thyroid Diseases; Carcinoma, Bronchogenic; Bronchial Neoplasms; Lung Neoplasms; Respiratory Tract Neoplasms; Thoracic Neoplasms; Lung Diseases; Respiratory Tract Diseases

Central Study Contacts

Sophia Paspal, Ph.D.

CONTACT

610-405-5974; Sophia.paspal@xynomicpharma.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 20, 2022
• First Posted: March 11, 2022
• Study Start: December 31, 2025
• Primary Completion (Estimated): December 30, 2027
• Study Completion (Estimated): December 30, 2028
• Last Updated: April 10, 2025

Record last verified: 2025-04