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.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
221
XP-102 will be administered orally once or twice daily in a continuous regimen.
Trametinib will be administered 2mg orally once a day.
Characterize the safety of XP-102.
Number of participants with treatment related adverse events.
Time frame: 28 days
Evaluate the pharmacokinetics of XP-102.
Blood plasma concentration.
Time frame: 28 days
Establish maximum tolerated dose of XP-102.
Number of participants with dose limiting toxicity
Time frame: 28 days
Evaluate the pharmacokinetics of XP-102 + trametinib.
Blood plasma concentration.
Time frame: 28 days
Characterize tolerability of XP-102 in combination with trametinib.
Number of participants with dose limiting toxicity
Time frame: 28 days
Evaluate the pharmacokinetics of XP-102 administered with food
Blood plasma concentration.
Time frame: 4 days
Evaluate clinical activity/efficacy of XP-102.
Overall Response Rate with RECIST criteria v1.1.
Time frame: Approximately every 8 weeks (up to 2 years)
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