A Study of Calderasib (MK-1084) in KRAS Mutant Advanced Solid Tumors (MK-1084-001)
- Summary
- This is a study evaluating the safety, pharmacokinetics, and efficacy of calderasib alone, and calderasib plus other combination therapies in participants with advanced solid tumors with identified kirsten rat sarcoma viral oncogene homolog G12C (KRAS G12C) mutation.
- Acronym
- KANDLELIT-001
- Short title
- A Study of Calderasib (MK-1084) in KRAS Mutant Advanced Solid Tumors (MK-1084-001)
- Official title
- A Phase 1, Open-label, Multicenter Study to Assess Safety, Tolerability, PK, and Efficacy of MK-1084 as Monotherapy and as Part of Various Combination Therapies in Participants With KRAS G12C Mutant Advanced Solid Tumors
- Control arm
- Open label
- Registry reports results
- Listing at source
- Listed
- Recruitment status
- Recruiting
- Phase
- Phase 1
- Study type
- Interventional
- Completion date
- 2030-02-25
- First posted
- 2021-10-05
- Registry last updated
- 2026-07-31
- Primary completion date
- 2030-02-25
- Start date
- 2021-12-17
- Participants
- Participant count basis
- Estimated
- Planned participants
- Protocol amendments
- Number of sites
- Data monitoring committee
- Registry sponsor category
- Industry
- Lead sponsor
- Merck Sharp & Dohme LLC
- Source registry
- ClinicalTrials.gov
- Registry ID
- NCT05067283
- ClinicalTrials.gov ID
- NCT05067283
- Registry record
- Open registry record
- Allocation
- Not randomised
- Model
- Parallel groups
- Purpose
- Treatment
- Masking
- No masking
Number of Participants Who Experience a Dose-Limiting Toxicity (DLT)
Timeframe: Up to ~21 days
A DLT is defined as an event with toxicity including the type, severity, time of onset, time of resolution, and the probable association with study treatment that are not due to pre-existing conditions as defined by the Common Terminology Criteria for Adverse Events Version 5.0 (CTCAE 5.0). Number of participants who experience a DLT will be reported.
Number of Participants Who Experience an Adverse Event (AE)
Timeframe: Up to ~56 months
An AE is any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product or protocol-specified procedure, whether or not considered related to the medicinal product or protocol-specified procedure. Any worsening of a preexisting condition that is temporally associated with the use of the Sponsor's product, is also an AE. The number of participants who experience an AE will be reported.
Number of Participants Who Discontinue Study Treatment Due to an AE
Timeframe: Up to ~56 months
An AE is any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product or protocol-specified procedure, whether or not considered related to the medicinal product or protocol-specified procedure. Any worsening of a preexisting condition that is temporally associated with the use of the Sponsor's product, is also an AE. The number of participants who discontinue study treatment due to an AE will be reported.
Objective Response Rate (ORR)
Timeframe: Up to ~56 months
ORR is defined as the percentage of participants who have a Complete Response (CR: Disappearance of all target lesions) or a Partial Response (PR: At least a 30% decrease in the sum of diameters of target lesions) per Response Evaluation Criteria in Solid Tumors 1.1 (RECIST 1.1). The percentage of participants who experience a CR or PR as assessed by the investigator based on RECIST 1.1 will be reported.
Duration of Response (DOR)
Timeframe: Up to ~56 months
DOR is defined as the time from first documented evidence of CR or PR until progressive disease (PD) or death. Per RECIST 1.1, PD is defined as at least a 20% increase in the sum of diameters of target lesions. In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. The appearance of one or more new lesions is also considered PD. The DOR as assessed by the investigator will be reported.
Mean Plasma Concentration of calderasib
Timeframe: At designated timepoints during the study in Cycles 1, 2, 3, 5, 9, 13, 17, 21, 25, and every 6 weeks thereafter up to 56 months. Cycle=3 weeks (Arms 1-4) and 4 weeks (Arms 5-6)
Mean Plasma Concentration of calderasib determined by blood samples collected pre-dose and at designated timepoints post-dose will be reported.
Maximum Concentration (Cmax) of calderasib
Timeframe: At designated timepoints during the study in Cycles 1, 2, 3, 5, 9, 13, 17, 21, 25, and every 6 weeks thereafter up to 56 months. Cycle=3 weeks (Arms 1-4) and 4 weeks (Arms 5-6).
Cmax of calderasib determined by blood samples collected pre-dose and at designated timepoints post-dose will be reported.
Time to Maximum Concentration (Tmax) of calderasib
Timeframe: At designated timepoints during the study in Cycles 1, 2, 3, 5, 9, 13, 17, 21, 25, and every 6 weeks thereafter up to 56 months. Cycle=3 weeks (Arms 1-4) and 4 weeks (Arms 5-6)
Tmax of calderasib determined by blood samples collected pre-dose and at designated timepoints post-dose will be reported.
Minimum Concentration (Cmin) of calderasib
Timeframe: At designated timepoints during the study in Cycles 1, 2, 3, 5, 9, 13, 17, 21, 25, and every 6 weeks thereafter up to 56 months. Cycle=3 weeks (Arms 1-4) and 4 weeks (Arms 5-6)
Cmin of calderasib determined by blood samples collected pre-dose and at designated timepoints post-dose will be reported.
Area Under the Concentration Time-Curve 0-12 Hours (AUC 0-12) of calderasib
Timeframe: At designated timepoint during the study in Cycle 1 Day 1: Predose and up to 12 hours postdose. Cycle=3 weeks (Arms 1-4) and 4 weeks (Arms 5-6)
AUC 0-12 of calderasib determined by blood samples collected pre-dose and at designated timepoints post-dose will be reported.
Area Under the Concentration Time-Curve 0-24 Hours (AUC 0-24) of calderasib
Timeframe: At designated timepoint during the study in Cycle 1 Day 1: Predose and up to 24 hours postdose. Cycle=3 weeks (Arms 1-4) and 4 weeks (Arms 5-6)
AUC 0-24 of calderasib determined by blood samples collected pre-dose and at designated timepoints post-dose will be reported.
Half-Life (t1/2) of calderasib
Timeframe: At designated timepoint during the study in Cycle 1 Day 1: Predose and up to 24 hours postdose. Cycle=3 weeks (Arms 1-4) and 4 weeks (Arms 5-6)
Half-Life (t1/2) of calderasib determined by blood samples collected pre-dose and at designated timepoints post-dose will be reported.
- Sex
- All
- Age groups
- Adults, Older adults
- Minimum age
- 18 Years
- Healthy volunteers
- No
For all participants:
- Has measurable disease by RECIST 1.1 criteria
- Has adequate organ function
- Male participants agree to protocol-specified contraception requirements including refraining from donating sperm and using protocol-specified contraceptives unless confirmed to be azoospermic
- Female participants must not be pregnant or breastfeeding, and must agree to protocol-specified contraceptive requirements and must have a negative highly sensitive pregnancy test within 24 hours (for a urine test) or 72 hours (for a serum test) before the first dose of study intervention
For Arm 1 - Has locally advanced unresectable or metastatic solid-tumor malignancy with histologically OR blood-based confirmation of KRAS G12C mutation who has received at least 1 line of therapy for systemic disease
For Arm 2
- Has an untreated metastatic non-small cell lung cancer (NSCLC) with histologically OR blood-based confirmation of KRAS G12C mutation and histologic confirmation of programmed cell death ligand 1 (PD-L1) tumor proportion score (TPS) ≥1%
For Arm 3
- Has locally advanced unresectable or metastatic solid-tumor malignancy with histological or blood-based confirmation of KRAS G12C mutation who has received at least 1 line of therapy for systemic disease Expansion Group A: 2L+NSCLC
- Has histologically or cytologically confirmed diagnosis of unresectable or metastatic NSCLC with histological or blood-based confirmation of KRAS G12C mutation and submits archival tumor sample
- Previous treatment failure of at least 1 line of systemic therapy Expansion Group B
- Has locally advanced unresectable or metastatic solid-tumor malignancy, excluding NSCLC or CRC, with histologically or blood- based confirmation of KRAS G12C mutation who has received at least 1 line of therapy for systemic disease
Arm 4 only - Has an untreated advanced or metastatic nonsquamous NSCLC with histologically or blood-based confirmation of KRAS G12C mutation
Arm 5 only
- Histologically or cytologically confirmed diagnosis of locally advanced unresectable or metastatic colorectal adenocarcinoma and with histologically or blood-based confirmation of KRAS G12C mutation
- Previous treatment failure of one or 2 previous line(s) of systemic therapy
Arm 6 only
- Locally advanced unresectable or metastatic colorectal adenocarcinoma with histologically or blood-based confirmation of KRAS G12C mutation
- Has received chemotherapy, definitive radiation, or biological cancer therapy within 4 weeks (2 weeks for palliative radiation) before first dose of study intervention
- Has a history of second malignancy, unless potentially curative treatment has been completed with no evidence of malignancy for 5 years
- Has clinically active central nervous system (CNS) metastases and/or carcinomatous meningitis
- Has an active infection requiring systemic therapy
- Known history of HIV infection or. has a known history of Hepatitis B virus or known active Hepatitis C virus infection
- Has a history of interstitial lung disease, noninfectious pneumonitis requiring active steroid therapy, or ongoing pneumonitis
- Has an active autoimmune disease requiring systemic therapy
- Has not fully recovered from any effects of major surgical procedure without significant detectable infection
- Has one or more of the following ophthalmological findings/conditions: intraocular pressure >21 mm Hg and/or any diagnosis of glaucoma; diagnosis of central serous retinopathy, retinal vein occlusion, or retinal artery occlusion and/or a diagnosis of retinal degenerative disease excluding age-related macular degeneration
- Has received live or live-attenuated vaccine within 4 weeks of study start
Arm 4 Only
- Is unable to interrupt aspirin or other nonsteroidal anti-inflammatories (NSAIDs), other than an aspirin dose ≤1.3 grams per day, for at least 2 days (5 days for long-acting agents [for example, piroxicam]) before, during, and for at least 2 days after administration of pemetrexed.
- Is unable/unwilling to take folic acid, vitamin B12, and dexamethasone
- Moffitt Cancer Center ( Site 0261)Tampa, United StatesRecruiting
- START Midwest ( Site 0267)Grand Rapids, United StatesRecruiting
- John Theurer Cancer Center at Hackensack University Medical Center ( Site 0260)Hackensack, United StatesRecruiting
- Laura and Isaac Perlmutter Cancer Center ( Site 0270)New York, United StatesCompleted
- NEXT Virginia ( Site 0271)Fairfax, United StatesRecruiting
- MEDICAL COLLEGE OF WISCONSIN-Cancer Center Clinical Trials Office ( Site 0262)Milwaukee, United StatesRecruiting
- Instituto Alexander Fleming ( Site 0434)Ciudad Autónoma de Buenos Aires, ArgentinaRecruiting
- Sanatorio Parque ( Site 0456)Rosario, ArgentinaRecruiting
- Fundación CORI para la Investigación y Prevención del Cáncer ( Site 0438)La Rioja, ArgentinaRecruiting
- Chris O'Brien Lifehouse ( Site 0002)Camperdown, AustraliaRecruiting
- Liverpool Hospital-Medical Oncology ( Site 0001)Liverpool, AustraliaRecruiting
- Westmead Hospital ( Site 0006)Westmead, AustraliaRecruiting
- Monash Health-Oncology Research ( Site 0003)Clayton, AustraliaRecruiting
- Cross Cancer Institute ( Site 0033)Edmonton, CanadaRecruiting
- The Moncton Hospital ( Site 0037)Moncton, CanadaRecruiting
- Hamilton Health Sciences-Juravinski Cancer Centre ( Site 0030)Hamilton, CanadaRecruiting
- Kingston Health Sciences Centre-Kingston General Hospital Site ( Site 0036)Kingston, CanadaRecruiting
- Princess Margaret Cancer Centre-Division of Medical Oncology and Hematology ( Site 0032)Toronto, CanadaRecruiting
- James Lind Centro de Investigacion del Cancer ( Site 0043)Temuco, ChileCompleted
- Centro de Estudios Clínicos SAGA-CECSAGA ( Site 0041)Santiago, ChileRecruiting
- FALP-UIDO ( Site 0040)Santiago, ChileRecruiting
- Bradfordhill ( Site 0042)Santiago, ChileRecruiting
- Beijing Friendship Hospital Affiliate of Capital University-Oncology ( Site 0417)Beijing, ChinaRecruiting
- Fujian Cancer Hospital ( Site 0419)Fuzhou, ChinaRecruiting
- Southern Medical University Nanfang Hospital-Depatrment of Respiratory and Critical Care Medicine ( Site 0413)Guangzhou, ChinaRecruiting
And 50 more, listed on the interactive page.
- PubMed 38924388Related publication
- Related resource (www.merckclinicaltrials.com)
- MK-1084-001
- U1111-1281-2482
- jRCT2041220034
- 2022-501563-40-00