^
    5d
    A Phase 1 Study to Assess Food Effect on the Pharmacokinetics of D3S-001 in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=26, Completed, D3 Bio (Wuxi) Co., Ltd | Recruiting --> Completed | N=14 --> 26
    Trial completion • Enrollment change
    |
    elisrasib (D3S-001)
    2ms
    Therapeutic advances with KRASG12C inhibitors and combination strategies in non-small cell lung cancer brain metastases. (PubMed, Cancer Gene Ther)
    This article examines the clinical and translational application of specific next-generation blood-brain barrier penetrant KRASG12C inhibitors, such as sotorasib, adagrasib, olomorasib, RMC-6236, and D3S-001, and their rational integration with radiation therapy, targeted therapies, and immunotherapies to overcome therapeutic resistance in patients with NSCLC brain metastases. This review summarizes recent advances aimed at enhancing intracranial tumor control and overall survival in patients with NSCLC brain metastases through the use of next-generation KRASG12C inhibitors and multimodal therapies.
    Review • Journal • IO biomarker
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    Lumakras (sotorasib) • Krazati (adagrasib) • daraxonrasib (RMC-6236) • elisrasib (D3S-001) • olomorasib (LY3537982)
    4ms
    A Phase 1/2 Study of D3S-002 as Monotherapy or Combination Therapy in Adult Subjects With Advanced Solid Tumors With MAPK Pathway Mutations (clinicaltrials.gov)
    P1/2, N=67, Active, not recruiting, D3 Bio (Wuxi) Co., Ltd | Phase classification: P1 --> P1/2 | Trial completion date: Nov 2025 --> Apr 2028 | Trial primary completion date: Nov 2025 --> Apr 2028
    Phase classification • Trial completion date • Trial primary completion date
    |
    D3S-002 • elisrasib (D3S-001)
    8ms
    A Phase 1 Study to Assess Food Effect on the Pharmacokinetics of D3S-001 in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=14, Recruiting, D3 Bio (Wuxi) Co., Ltd
    New P1 trial
    |
    elisrasib (D3S-001)
    10ms
    D3S-001-100: A Study of D3S 001 Monotherapy or Combination Therapy in Subjects With Advanced Solid Tumors With a KRAS p.G12C Mutation (clinicaltrials.gov)
    P1/2, N=442, Recruiting, D3 Bio (Wuxi) Co., Ltd | Trial completion date: Sep 2026 --> Feb 2027 | Trial primary completion date: Sep 2026 --> Feb 2027
    Trial completion date • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Keytruda (pembrolizumab) • Erbitux (cetuximab) • cisplatin • carboplatin • pemetrexed • elisrasib (D3S-001)
    11ms
    D3S-001 in advanced solid tumors with KRASG12C mutations: a phase 1 trial. (PubMed, Nat Med)
    The phase 1b expansion phase is ongoing. ClinicalTrials.gov identifier: NCT05410145 .
    P1 data • Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    elisrasib (D3S-001)
    almost2years
    D3S-001, a KRAS G12C inhibitor with rapid target engagement kinetics, overcomes nucleotide cycling and demonstrates robust preclinical and clinical activities. (PubMed, Cancer Discov)
    In the presence of growth factors, such as EGF and HGF, the ability of sotorasib and adagrasib to inhibit KRAS was compromised whereas the TE kinetics of D3S-001 was nearly unaffected, a unique feature differentiating D3S-001 from other GDP-bound G12C inhibitors. Furthermore, the high covalent potency and cellular TE efficiency of D3S-001 contributed to robust anti-tumor activity preclinically and translated into promising clinical activity in an ongoing phase 1 trial (NCT05410145).
    Preclinical • Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Lumakras (sotorasib) • Krazati (adagrasib) • elisrasib (D3S-001)
    almost2years
    A Study of D3S 001 Monotherapy or Combination Therapy in Subjects With Advanced Solid Tumors With a KRAS p.G12C Mutation (clinicaltrials.gov)
    P1/2, N=352, Recruiting, D3 Bio (Wuxi) Co., Ltd | Phase classification: P1 --> P1/2 | N=168 --> 352 | Trial completion date: May 2025 --> Sep 2026 | Trial primary completion date: May 2025 --> Sep 2026
    Phase classification • Enrollment change • Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Keytruda (pembrolizumab) • Erbitux (cetuximab) • cisplatin • carboplatin • pemetrexed • elisrasib (D3S-001)
    over2years
    A Study of D3S-001 as Monotherapy in Subjects With Advanced Solid Tumors With a KRAS p.G12C Mutation (clinicaltrials.gov)
    P1, N=168, Recruiting, D3 Bio (Wuxi) Co., Ltd
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    elisrasib (D3S-001)
    3years
    A Study of D3S-001 as Monotherapy in Subjects With Advanced Solid Tumors With a KRAS p.G12C Mutation (clinicaltrials.gov)
    P1, N=168, Recruiting, D3 Bio (Wuxi) Co., Ltd | N=98 --> 168
    Enrollment change • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    elisrasib (D3S-001)