A First-in-human Study of RLY-8161 in Advanced NRAS-Mutant Solid Tumors

Trial statusRecruiting
Trial phasePhase 1
Trial typeInterventional
Biological sexAll
Age18+
SponsorRelay Therapeutics, Inc.

About this trial

This is a Phase 1 first-in-human, open-label multicenter study designed to evaluate the safety, tolerability, pharmacokinetics (PK), pharmacodynamics, and preliminary antitumor activity of RLY-8161, an NRAS-selective inhibitor, in participants with advanced NRAS-mutant melanoma and other solid tumors.

Eligibility criteria

This trial does not accept healthy volunteers

Qualifiers

Eastern Cooperative Oncology Group (ECOG) performance status of 0 to 1.

Histologically confirmed diagnosis of unresectable Stage III or IV melanoma or other solid tumor.

Disease is refractory to standard therapy (including targeted therapy), participant is intolerant of standard therapy, or participant has declined standard therapy.

Measurable disease per Response Evaluation Criteria in Solid Tumors (RECIST) v1.1.

Disqualifiers

Known activating KRAS, HRAS, or BRAF mutation or known alterations in other driver oncogenes.

Prior treatment with ERK, MEK, RAF, or RAS targeting agents or any agent whose mechanism of action is to inhibit the RAS-MAPK pathway.

For participants with melanoma: lactate dehydrogenase (LDH) >2×ULN.

Central nervous system (CNS) metastases that are associated with progressive neurologic symptoms or require ongoing corticosteroids to control the CNS disease.

Trial design

Design model

Sequential

Treatments tested in this trial

  • RLY-8161

    Drug

    RLY-8161 is an NRAS-selective inhibitor

Treatment groups

35 Participants
are divided into 2 treatment groups
Group A: Part 1: RLY-8161 for participants with advanced NRAS-mutant solid tumorsExperimental treatment 1 intervention
Group B: Part 2: RLY-8161 for participants with advanced NRAS-mutant solid tumorsExperimental treatment 1 intervention

Trial outcomes

Primary outcomes

1

Part 1: Maximum Tolerated Dose (MTD) and/or RP2D of RLY-8161

Time frame
Cycle 1 (28-day cycle) of treatment for MTD and at the end of every cycle (28-day cycle) for RP2D until treatment discontinuation, approximately 12 months
2

Part 1: Number of participants with Adverse Events (AEs) or Serious Adverse Events (SAEs), with changes in vital signs, electrocardiograms (ECGs), and laboratory tests

Time frame
Cycle 1 (28-day cycle) of treatment and at the end of every cycle (28-day cycle) until 30 days after treatment discontinuation, approximately 13 months
3

Part 2: Objective Response Rate (ORR) of RLY-8161 as assessed by RECIST v1.1

Time frame
Approximately every 8 weeks on treatment and every 12 weeks after last dose in the absence of progressive disease, approximately 18 months

Secondary outcomes

1

Part 1 and Part 2: Changes in NRAS mutant allele fraction in ctDNA

Time frame
Approximately every 2 weeks in Cycle 1 (28-day cycle), at the beginning of Cycle 2 (28-day cycle), and at the beginning of every odd cycle (28-day cycle) until End of Treatment (EOT), approximately 12 months
2

Part 1 and Part 2: Plasma concentration and PK parameters of RLY-8161

Time frame
Approximately every 2 weeks in Cycle 1 (28-day cycle) and at Day 1 of every cycle (28-day cycle) through Cycle 4
3

Part 1: ORR of RLY-8161 as assessed by RECIST v1.1

Time frame
Approximately every 8 weeks on treatment and every 12 weeks after last dose in the absence of progressive disease, approximately 18 months
4

Part 1 and 2: Duration of Response (DOR) of RLY-8161 as assessed by RECIST v1.1

Time frame
Approximately every 8 weeks on treatment and every 12 weeks after last dose in the absence of progressive disease, approximately 18 months

Other outcomes

Sponsors and contacts

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