This Phase 1/2, first-in-human, open-label, multicenter study follows a 3+3 ascending dose escalation design to determine the MTD/RP2D and to characterize the safety, tolerability, PK, and antitumor effects of LNS8801 alone and in combination with pembrolizumab. The study will include a dose escalation phase, a dose expansion phase, and phase 2A cohorts. Up to 200 patients will be accrued for this study. Up to 15 study sites in the United States will participate in the study.
Has histopathologically confirmed locally advanced or metastatic solid tumor cancer.
Is able to understand and voluntarily sign a written informed consent form and is willing and able to comply with protocol requirements.
Is considered likely to meet the detailed inclusion and
Having received anti-PD-1/L1 therapy at least twice if dosed every 4 weeks (q4w) or longer, at least 3 times if dosed every 3 weeks (q3w), or at least 4 times if dosed every 2 weeks (q2w) and,
Having documented clinical or radiographic progression of disease (PD) while on anti-PD-1/L1 therapy.
Has no standard of care or the patient declines standard of care options.
Has measurable disease per RECIST v1.1 or RANO as assessed by the local site investigator/radiologist. Lesions in a previously irradiated area are measurable if progression has been demonstrated after radiation. Lesions must be measurable in at least 2 dimensions in a spiral CT scan or MRI. For lymphoma patients only, the minimum measurement must be >15 mm on the long axis and >10 mm on the short axis.
Single group
LNS8801 -Small molecule, orally bioavailable, selective agonist of GPER
DrugLNS8801 -Small molecule, orally bioavailable, selective agonist of GPER
Pembrolizumab - anti-PD-1 antibody
Biological/Vaccinepembrolizumab- anti-PD-1 antibody
Adverse events observed for LNS8801 dosed alone and in combination with pembrolizumab
LNS8801 plasma exposure (AUC) as a function of dose
AUC0-end
LNS8801 plasma exposure (Cmax) as a function of dose
Cmax
LNS8801 plasma exposure (t1/2) as a function of dose
T1/2
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Linnaeus Therapeutics, Inc.
Lead sponsor
Merck Sharp & Dohme LLC
Collaborator
