^
    19d
    KANDLELIT-001: A Study of Calderasib (MK-1084) in KRAS Mutant Advanced Solid Tumors (MK-1084-001) (clinicaltrials.gov)
    P1, N=830, Recruiting, Merck Sharp & Dohme LLC | N=167 --> 830
    Enrollment change
    |
    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Keytruda (pembrolizumab) • Erbitux (cetuximab) • carboplatin • 5-fluorouracil • pemetrexed • oxaliplatin • leucovorin calcium • calderasib (MK-1084)
    19d
    KANDLELIT-013: MK-3475A±Calderasib (MK-1084) in Completely Resected Stage IIA-IIIB (N2) KRAS G12Cm NSCLC (MK-1084-013) (clinicaltrials.gov)
    P3, N=400, Recruiting, Merck Sharp & Dohme LLC | N=102 --> 400
    Enrollment change • Trial initiation date
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Keytruda (pembrolizumab) • calderasib (MK-1084)
    20d
    A Clinical Trial of Calderasib (MK-1084) and Durvalumab in People With Non-Small Cell Lung Cancer (MK-1084-015/KANDLELIT-015) (clinicaltrials.gov)
    P3, N=310, Not yet recruiting, Merck Sharp & Dohme LLC
    New P3 trial
    |
    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Imfinzi (durvalumab) • calderasib (MK-1084)
    20d
    KANDLELIT-014: A Clinical Study of Calderasib (MK-1084) in People With Advanced Solid Tumors (MK-1084-014) (clinicaltrials.gov)
    P2, N=150, Recruiting, Merck Sharp & Dohme LLC
    Trial initiation date • Pan tumor
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Erbitux (cetuximab) • calderasib (MK-1084)
    22d
    A clinical trial of MK-1084, pembrolizumab, and chemotherapy in people with nonsmall cell lung cancer (MK-1084-013) (2024-517337-41-00)
    P2/3, N=79, Not yet recruiting, Merck Sharp & Dohme LLC
    New P2/3 trial
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Keytruda (pembrolizumab) • cisplatin • carboplatin • pemetrexed • calderasib (MK-1084)
    1m
    KANDLELIT-001: A Study of Calderasib (MK-1084) in KRAS Mutant Advanced Solid Tumors (MK-1084-001) (clinicaltrials.gov)
    P1, N=167, Recruiting, Merck Sharp & Dohme LLC | N=126 --> 167
    Enrollment change
    |
    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Keytruda (pembrolizumab) • Erbitux (cetuximab) • carboplatin • 5-fluorouracil • pemetrexed • oxaliplatin • leucovorin calcium • calderasib (MK-1084)
    1m
    From KRASG12D to Pan-KRAS Inhibitors─A Journey Enabled by Synthetic Innovation and Structure-Based Drug Design. (PubMed, J Med Chem)
    KRAS, a significant oncology target, has been challenging to develop drugs for until recent discoveries of KRASG12C mutant-specific covalent inhibitors, including MK-1084. This article describes efforts toward the discovery of KRASG12D mutant-specific inhibitors and how synthetic innovations and structure-based drug design were utilized to facilitate the discovery of pan-KRAS inhibitors.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12D
    |
    calderasib (MK-1084)
    2ms
    KANDLELIT-013: MK-3475A±MK-1084 in Completely Resected Stage IIA-IIIB (N2) KRAS G12Cm NSCLC (MK-1084-013) (clinicaltrials.gov)
    P3, N=400, Recruiting, Merck Sharp & Dohme LLC | Not yet recruiting --> Recruiting
    Enrollment open
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Keytruda (pembrolizumab) • calderasib (MK-1084)
    2ms
    KEYMAKER-U01 Substudy 01J: A Study of Pembrolizumab Plus MK-1084 in Participants With Non-Small Cell Lung Cancer (NSCLC) With Kirsten Rat Sarcoma Viral Oncogene Homolog (KRAS) G12C Mutations (MK-3475-01J/KEYMAKER-U01J) (clinicaltrials.gov)
    P2, N=130, Recruiting, Merck Sharp & Dohme LLC
    Trial initiation date
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Keytruda (pembrolizumab) • Erbitux (cetuximab) • carboplatin • pemetrexed • calderasib (MK-1084)
    2ms
    A Clinical Study of MK-1084 With Other Treatments for Non-small Cell Lung Cancer (MK-3475-01F) (clinicaltrials.gov)
    P1/2, N=190, Recruiting, Merck Sharp & Dohme LLC | N=57 --> 190
    Enrollment change • Trial initiation date
    |
    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Keytruda (pembrolizumab) • Erbitux (cetuximab) • patritumab deruxtecan (U3-1402) • Jiataile (sacituzumab tirumotecan) • calderasib (MK-1084)
    2ms
    A Clinical Study of Calderasib (MK-1084) and Other Treatments for Participants With Non-Small Cell Lung Cancer (MK-1084-007/KANDLELIT-007) (clinicaltrials.gov)
    P3, N=675, Recruiting, Merck Sharp & Dohme LLC | N=218 --> 675
    Enrollment change • Trial initiation date
    |
    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase)
    |
    Keytruda (pembrolizumab) • cisplatin • carboplatin • pemetrexed • calderasib (MK-1084)
    2ms
    A Clinical Study of MK-1084 With Other Treatments for Non-small Cell Lung Cancer (MK-3475-01F) (clinicaltrials.gov)
    P1/2, N=57, Recruiting, Merck Sharp & Dohme LLC | N=32 --> 57
    Enrollment change
    |
    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Keytruda (pembrolizumab) • Erbitux (cetuximab) • patritumab deruxtecan (U3-1402) • Jiataile (sacituzumab tirumotecan) • calderasib (MK-1084)