^
    18h
    KontRASt-02: Study of JDQ443 in Comparison With Docetaxel in Participants With Locally Advanced or Metastatic KRAS G12C Mutant Non-small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=95, Active, not recruiting, Novartis Pharmaceuticals | Trial primary completion date: Sep 2024 --> May 2025
    Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    docetaxel • opnurasib (JDQ443)
    14d
    KontRASt-01: Study of JDQ443 in Patients With Advanced Solid Tumors Harboring the KRAS G12C Mutation (clinicaltrials.gov)
    P1/2, N=344, Active, not recruiting, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting | Trial completion date: Jan 2027 --> Mar 2026 | Trial primary completion date: Jan 2027 --> Mar 2026
    Enrollment closed • Trial completion date • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Tevimbra (tislelizumab-jsgr) • batoprotafib (TNO155) • opnurasib (JDQ443)
    1m
    A Phase II Study of Neoadjuvant Opnurasib KRAS G12C Inhibitor in Patients With Surgically Resectable Non-Small Cell Lung Cancer (CCTG IND.242A): A Substudy of the IND.242 Platform Master Protocol. (PubMed, Clin Lung Cancer)
    Secondary objectives include safety and tolerability of the treatment regimen, objective response rate (ORR) by RECIST 1.1 for the neoadjuvant treatment period, pathological complete response (pCR) rate, event-free survival (EFS) at 2 years, and surgical outcomes. Exploratory objectives are to explore patient related outcomes (PROs) and identify potential predictive biomarkers of response and mechanisms of resistance on tissue and peripheral blood samples.
    P2 data • Journal
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • ALK (Anaplastic lymphoma kinase)
    |
    KRAS mutation
    |
    opnurasib (JDQ443)
    1m
    A Phase 1 Study to Evaluate the Pharmacokinetics of JDQ443 in Participants With Hepatic Impairment Compared to Matched Healthy Control Participants. (clinicaltrials.gov)
    P1, N=33, Terminated, Novartis Pharmaceuticals | N=48 --> 33 | Trial completion date: Aug 2024 --> Apr 2024 | Recruiting --> Terminated | Trial primary completion date: Aug 2024 --> Apr 2024; Sponsor Decision
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
    |
    opnurasib (JDQ443)
    2ms
    KontRASt-03: Platform Study of JDQ443 in Combinations in Patients With Advanced Solid Tumors Harboring the KRAS G12C Mutation (clinicaltrials.gov)
    P1/2, N=74, Active, not recruiting, Novartis Pharmaceuticals | N=346 --> 74
    Enrollment change • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Erbitux (cetuximab) • Mekinist (trametinib) • Kisqali (ribociclib) • opnurasib (JDQ443)
    4ms
    KontRASt-03: Platform Study of JDQ443 in Combinations in Patients With Advanced Solid Tumors Harboring the KRAS G12C Mutation (clinicaltrials.gov)
    P1/2, N=346, Active, not recruiting, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting | Trial completion date: Jun 2027 --> May 2025 | Trial primary completion date: May 2027 --> Mar 2025
    Enrollment closed • Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Erbitux (cetuximab) • Mekinist (trametinib) • Kisqali (ribociclib) • opnurasib (JDQ443)
    5ms
    KontRASt-02: Study of JDQ443 in Comparison With Docetaxel in Participants With Locally Advanced or Metastatic KRAS G12C Mutant Non-small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=95, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Dec 2025 --> May 2025 | Trial primary completion date: Apr 2025 --> Sep 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    docetaxel • opnurasib (JDQ443)
    5ms
    KontRASt-02: Study of JDQ443 in Comparison With Docetaxel in Participants With Locally Advanced or Metastatic KRAS G12C Mutant Non-small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=95, Active, not recruiting, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting | N=360 --> 95
    Enrollment closed • Enrollment change • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    docetaxel • opnurasib (JDQ443)
    6ms
    STRIDER: JDQ443 for KRAS G12C NSCLC Brain Metastases (clinicaltrials.gov)
    P2, N=0, Withdrawn, Maastricht University Medical Center | N=42 --> 0 | Not yet recruiting --> Withdrawn
    Enrollment change • Trial withdrawal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    opnurasib (JDQ443)
    6ms
    Study of Efficacy and Safety of JDQ443 Single-agent as First-line Treatment for Patients With Locally Advanced or Metastatic KRAS G12C- Mutated Non-small Cell Lung Cancer With a PD-L1 Expression < 1% or a PD-L1 Expression ≥ 1% and an STK11 Co-mutation. (clinicaltrials.gov)
    P2, N=96, Active, not recruiting, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • STK11 (Serine/threonine kinase 11)
    |
    PD-L1 expression • KRAS mutation • KRAS G12C • STK11 mutation • KRAS G12 • KRAS G12C + PD-L1 expression
    |
    opnurasib (JDQ443)
    6ms
    ABCB1 attenuates brain exposure to the KRASG12C inhibitor opnurasib whereas binding to mouse carboxylesterase 1c influences its plasma exposure. (PubMed, Biomed Pharmacother)
    Opnurasib (JDQ443) is a newly developed oral KRASG12C inhibitor, with a binding mechanism distinct from the registered KRASG12C inhibitors sotorasib and adagrasib...The Abcb1a/b transporter activity could be almost completely reversed by co-administration of elacridar, a dual ABCB1/ABCG2 inhibitor, increasing the brain penetration without any behavioral or postural signs of acute CNS-related toxicity...Plasma Ces1c therefore likely binds opnurasib, increasing its retention in plasma. The obtained pharmacokinetic insights may be useful for further optimization of the clinical efficacy and safety of opnurasib, and might reveal potential drug-drug interaction risks.
    Preclinical • Journal
    |
    KRAS (KRAS proto-oncogene GTPase) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • SLCO1C1 (Solute Carrier Organic Anion Transporter Family Member 1C1)
    |
    Lumakras (sotorasib) • Krazati (adagrasib) • elacridar (GF120918) • opnurasib (JDQ443)
    8ms
    STRIDER: JDQ443 for KRAS G12C NSCLC Brain Metastases (clinicaltrials.gov)
    P2, N=42, Not yet recruiting, Maastricht University Medical Center | Initiation date: Nov 2023 --> Apr 2024
    Trial initiation date
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    opnurasib (JDQ443)
    9ms
    A Phase 1 Study to Evaluate the Pharmacokinetics of JDQ443 in Participants With Hepatic Impairment Compared to Matched Healthy Control Participants. (clinicaltrials.gov)
    P1, N=48, Recruiting, Novartis Pharmaceuticals | Active, not recruiting --> Recruiting | N=30 --> 48
    Enrollment open • Enrollment change
    |
    opnurasib (JDQ443)
    10ms
    A Phase 1 Study to Evaluate the Pharmacokinetics of JDQ443 in Participants With Hepatic Impairment Compared to Matched Healthy Control Participants. (clinicaltrials.gov)
    P1, N=30, Active, not recruiting, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    opnurasib (JDQ443)
    11ms
    Development and validation of an LC-MS/MS method for the quantification of KRAS inhibitor opnurasib in several mouse matrices and its application in a pharmacokinetic mouse study. (PubMed, J Chromatogr B Analyt Technol Biomed Life Sci)
    Erlotinib was used as internal standard and acetonitrile was utilized to treat 10 µl of the sample with protein precipitation in a 96-well plate format. Opnurasib in mouse plasma was stable up to 12 h at room temperature, and up to 8 h at room temperature in tissue homogenates (except for kidney up to 4 h). This presented method has been successfully applied to quantify opnurasib in preclinical samples from a mouse study and demonstrated its usability to support preclinical pharmacokinetic studies.
    PK/PD data • Preclinical • Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    erlotinib • opnurasib (JDQ443)
    11ms
    KontRASt-01 Update: Safety and Efficacy of JDQ443 in KRAS G12C-Mutated Solid Tumors Including Non-Small Cell Lung Cancer (NSCLC) (MTCS 2023)
    JDQ443 demonstrates an acceptable safety and tolerability profile at 200 mg BID, with clinical activity in pts with NSCLC. Enrollment is ongoing to the JDQ443 monotherapy DEx and the JDQ443 + TNO155 and JDQ443 + tislelizumab combination arms.
    Clinical • PD(L)-1 Biomarker • IO biomarker
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Tevimbra (tislelizumab-jsgr) • batoprotafib (TNO155) • opnurasib (JDQ443)
    11ms
    KontRASt-02: A Phase III Trial Investigating the Efficacy and Safety of the KRASG12C Inhibitor JDQ443 vs. Docetaxel in Patients with Previously Treated, Locally Advanced or Metastatic, KRAS G12C-Mutated NSCLC (MTCS 2023)
    TBD
    Clinical • P3 data • IO biomarker • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    docetaxel • opnurasib (JDQ443)
    11ms
    A Phase II Trial of JDQ443 in KRAS G12C-Mutated NSCLC with PD-L1 Expression <1% or PD-L1 Expression ≥1% and an STK11 Co-Mutation (MTCS 2023)
    TBD
    P2 data • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • STK11 (Serine/threonine kinase 11)
    |
    PD-L1 expression • KRAS mutation • KRAS G12C • STK11 mutation • KRAS G12 • KRAS mutation + STK11 mutation • KRAS G12C + PD-L1 expression • PD-L1 expression + STK11 mutation
    |
    opnurasib (JDQ443)
    1year
    CRISPR screening identifies mechanisms of resistance to KRASG12C and SHP2 inhibitor combinations in non-small cell lung cancer. (PubMed, Cancer Res)
    To identify rational combination strategies that could help overcome or prevent some types of resistance, we evaluated the duration of tumor responses to JDQ443 ± TNO155, alone or combined with the PI3Kα inhibitor alpelisib and/or the CDK4/6 inhibitor ribociclib, in xenograft models derived from a KRASG12C-mutant NSCLC line and investigated the genetic mechanisms associated with loss of response to combined KRASG12C/SHP2 inhibition. Overall, KRAS G12C amplification and alterations of the MAPK/PI3K pathway were predominant mechanisms of resistance to combined KRASG12C/SHP2 inhibitors in preclinical settings. The biological nodes identified by CRISPR screening might provide additional starting points for effective combination treatments.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
    |
    KRAS mutation • KRAS G12C
    |
    Piqray (alpelisib) • Kisqali (ribociclib) • batoprotafib (TNO155) • opnurasib (JDQ443)
    1year
    A Phase 1 Study to Evaluate the Pharmacokinetics of JDQ443 in Participants With Hepatic Impairment Compared to Matched Healthy Control Participants. (clinicaltrials.gov)
    P1, N=48, Recruiting, Novartis Pharmaceuticals | Suspended --> Recruiting
    Enrollment open
    |
    opnurasib (JDQ443)
    1year
    KontRASt-01 update: Safety and efficacy of JDQ443 in KRAS G12C-mutated solid tumors including non-small cell lung cancer (NSCLC) (DGHO 2023)
    JDQ443 demonstrates an acceptable safety and tolerability profile at 200 mg BID, with clinical activity in NSCLC pts. Enrollment is ongoing to the JDQ443 monotherapy DEx and the JDQ443+TNO155 and JDQ443+tislelizumab arms.
    Clinical • PD(L)-1 Biomarker • IO biomarker
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Tevimbra (tislelizumab-jsgr) • batoprotafib (TNO155) • opnurasib (JDQ443)
    1year
    STRIDER: JDQ443 for KRAS G12C NSCLC Brain Metastases (clinicaltrials.gov)
    P2, N=42, Not yet recruiting, Maastricht University Medical Center
    New P2 trial
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    opnurasib (JDQ443)
    over1year
    KontRASt-01: Preliminary Safety and Efficacy of JDQ443 + TNO155 in Patients with Advanced, KRAS G12C-Mutated Solid Tumors (IASLC-WCLC 2023)
    JDQ443+TNO155 was tolerated with notable toxicities of edema, cytopenias, and fatigue. MTD was not reached; the RD for further evaluation was selected based on collective safety, pharmacokinetics, and efficacy. Preliminary anti-tumor activity was observed, including in KRASG12C inhibitor previously-treated NSCLC.
    Clinical • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    batoprotafib (TNO155) • opnurasib (JDQ443)
    over1year
    KontRASt-02: Study of JDQ443 in Comparison With Docetaxel in Participants With Locally Advanced or Metastatic KRAS G12C Mutant Non-small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=360, Recruiting, Novartis Pharmaceuticals | Trial completion date: May 2025 --> Dec 2025
    Trial completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    docetaxel • opnurasib (JDQ443)
    over1year
    KontRASt-03: Platform Study of JDQ443 in Combinations in Patients With Advanced Solid Tumors Harboring the KRAS G12C Mutation (clinicaltrials.gov)
    P1/2, N=346, Recruiting, Novartis Pharmaceuticals | Trial completion date: Aug 2025 --> Jun 2027 | Trial primary completion date: Jun 2025 --> May 2027
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Erbitux (cetuximab) • Mekinist (trametinib) • Kisqali (ribociclib) • opnurasib (JDQ443)
    over1year
    Neoadjuvant Platform Trial in Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=27, Recruiting, Canadian Cancer Trials Group | Not yet recruiting --> Recruiting
    Enrollment open
    |
    opnurasib (JDQ443)
    over1year
    KontRASt-01: Study of JDQ443 in Patients With Advanced Solid Tumors Harboring the KRAS G12C Mutation (clinicaltrials.gov)
    P1/2, N=475, Recruiting, Novartis Pharmaceuticals | Trial completion date: May 2025 --> Jan 2027 | Trial primary completion date: May 2025 --> Jan 2027
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Tevimbra (tislelizumab-jsgr) • batoprotafib (TNO155) • opnurasib (JDQ443)
    over1year
    Neoadjuvant Platform Trial in Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=27, Not yet recruiting, Canadian Cancer Trials Group | Initiation date: Jan 2023 --> May 2023
    Trial initiation date
    |
    opnurasib (JDQ443)
    over1year
    A phase II trial of JDQ443 in KRAS G12C-mutated NSCLC with PD-L1 expression <1% or PD-L1 expression ≥1% and an STK11 co-mutation. (ASCO 2023)
    Reused with permission. Clinical trial information: NCT05445843.
    P2 data • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • STK11 (Serine/threonine kinase 11)
    |
    PD-L1 expression • KRAS mutation • KRAS G12C • STK11 mutation • KRAS G12 • KRAS mutation + STK11 mutation • PD-L1 expression + STK11 mutation
    |
    opnurasib (JDQ443)
    over1year
    KontRASt-02: A phase III trial investigating the efficacy and safety of the KRASG12C inhibitor JDQ443 vs docetaxel in patients with previously treated, locally advanced or metastatic, KRAS G12C-mutated NSCLC. (ASCO 2023)
    The KontRASt-02 study is currently enrolling pts. Clinical trial information: NCT05132075.
    Clinical • P3 data • IO biomarker • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    docetaxel • opnurasib (JDQ443)
    over1year
    KontRASt-01 update: Safety and efficacy of JDQ443 in KRAS G12C-mutated solid tumors including non-small cell lung cancer (NSCLC). (ASCO 2023)
    JDQ443 demonstrates an acceptable safety and tolerability profile at 200 mg BID, with clinical activity in pts with NSCLC. Enrollment is ongoing to the JDQ443 monotherapy DEx and the JDQ443 + TNO155 and JDQ443 + tislelizumab combination arms. Clinical trial information: NCT04699188.
    Clinical • PD(L)-1 Biomarker • IO biomarker
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Tevimbra (tislelizumab-jsgr) • batoprotafib (TNO155) • opnurasib (JDQ443)
    over1year
    KontRASt-02: Study of JDQ443 in Comparison With Docetaxel in Participants With Locally Advanced or Metastatic KRAS G12C Mutant Non-small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=360, Recruiting, Novartis Pharmaceuticals | Trial completion date: Jan 2025 --> May 2025 | Trial primary completion date: Jan 2025 --> Apr 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    docetaxel • opnurasib (JDQ443)
    over1year
    Chromatin modification driving sub-clonal resistance to KRAS G12C combination therapies in KRAS mutant non-small cell lung cancer (AACR 2023)
    However, not all patients respond (sotorasib - ORR = 37.1%, adagrasib - 43%, JDQ443 - 35%), motivating preclinical and clinical investigation into mechanisms of intrinsic and acquired resistance. Moreover, we observed distinct persister subpopulations with resistance to KRAS G12Ci combination co-targeting orthogonal pathways (SHP2, CDK4/6, PI3K, and MCL-1), raising the possibility that distinct epigenetic-transcriptional states contribute to differential drug response and clonal evolution of persisters. Collectively, these results suggest that more complete tumor regression may be achieved by orthogonal strategies that target different resistant populations within the same tumor.
    Combination therapy
    |
    KRAS (KRAS proto-oncogene GTPase) • CDK4 (Cyclin-dependent kinase 4)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Lumakras (sotorasib) • Krazati (adagrasib) • opnurasib (JDQ443)
    over1year
    The combination of ulixertinib (ERK1/2 Inhibitor) and KRASG12C inhibition demonstrates significant efficacy in preclinical models (AACR 2023)
    KRASG12C mutant-inhibitors, including AMG-510 (sotorasib), MRTX849 (adagrasib), and JDQ443 have demonstrated efficacy in KRASG12C-mutant cancers, including NSCLC. Expression of the mutant KRAS alleles were readily confirmed from RNA sequencing data in all models. Gene expression analysis showed differential expression of MAPK pathway genes in monotherapy versus combination therapy treated groups.In summary, ulixertinib combined with adagrasib exhibited robust pre-clinical activity in a variety of xenograft models with KRASG12C and should be further evaluated.
    Preclinical
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS expression
    |
    Lumakras (sotorasib) • Krazati (adagrasib) • ulixertinib (BVD-523) • opnurasib (JDQ443)
    over1year
    A Phase II trial of JDQ443 in KRAS G12C-mutated NSCLC with PD-L1 expression <1% or PD-L1 expression≥1% and an STK11 co-mutation (AACR 2023)
    Other secondary endpoints include progression-free survival, overall survival, safety, pharmacokinetics, and pt-reported outcomes. A comprehensive biomarker strategy aims to investigate predictors of treatment response and resistance in the study population.
    P2 data • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • STK11 (Serine/threonine kinase 11)
    |
    PD-L1 expression • KRAS mutation • KRAS G12C • STK11 mutation • KRAS G12 • KRAS mutation + STK11 mutation • PD-L1 expression + STK11 mutation
    |
    opnurasib (JDQ443)
    almost2years
    KontRASt-02: Study of JDQ443 in Comparison With Docetaxel in Participants With Locally Advanced or Metastatic KRAS G12C Mutant Non-small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=360, Recruiting, Novartis Pharmaceuticals | Trial completion date: May 2025 --> Jan 2025 | Trial primary completion date: Aug 2024 --> Jan 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    docetaxel • opnurasib (JDQ443)
    almost2years
    KontRASt-01: Study of JDQ443 in Patients With Advanced Solid Tumors Harboring the KRAS G12C Mutation (clinicaltrials.gov)
    P1/2, N=375, Recruiting, Novartis Pharmaceuticals | Trial completion date: Aug 2024 --> May 2025 | Trial primary completion date: Aug 2024 --> May 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Tevimbra (tislelizumab-jsgr) • batoprotafib (TNO155) • opnurasib (JDQ443)
    almost2years
    KontRASt-03: Platform Study of JDQ443 in Combinations in Patients With Advanced Solid Tumors Harboring the KRAS G12C Mutation (clinicaltrials.gov)
    P1/2, N=346, Recruiting, Novartis Pharmaceuticals | Initiation date: Jan 2022 --> Oct 2022
    Trial initiation date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Erbitux (cetuximab) • Mekinist (trametinib) • Kisqali (ribociclib) • opnurasib (JDQ443)
    almost2years
    KontRASt-03: Platform Study of JDQ443 in Combinations in Patients With Advanced Solid Tumors Harboring the KRAS G12C Mutation (clinicaltrials.gov)
    P1/2, N=346, Recruiting, Novartis Pharmaceuticals | Initiation date: Oct 2022 --> Jan 2022
    Trial initiation date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Erbitux (cetuximab) • Mekinist (trametinib) • Kisqali (ribociclib) • opnurasib (JDQ443)
    almost2years
    Study of Efficacy and Safety of JDQ443 Single-agent as First-line Treatment for Patients With Locally Advanced or Metastatic KRAS G12C- Mutated Non-small Cell Lung Cancer With a PD-L1 Expression < 1% or a PD-L1 Expression ≥ 1% and an STK11 Co-mutation. (clinicaltrials.gov)
    P2, N=120, Recruiting, Novartis Pharmaceuticals | Not yet recruiting --> Recruiting
    Enrollment open • IO biomarker • Metastases
    |
    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • STK11 (Serine/threonine kinase 11)
    |
    PD-L1 expression • KRAS mutation • KRAS G12C • STK11 mutation • KRAS G12
    |
    opnurasib (JDQ443)
    almost2years
    JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS for the Treatment of Solid Tumors. (PubMed, J Med Chem)
    JDQ443 showed PK/PD activity in vivo and dose-dependent antitumor activity in mouse xenograft models. JDQ443 is now in clinical development, with encouraging early phase data reported from an ongoing Phase Ib/II clinical trial (NCT04699188).
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    opnurasib (JDQ443)
    2years
    KontRASt-03: Platform Study of JDQ443 in Combinations in Patients With Advanced Solid Tumors Harboring the KRAS G12C Mutation (clinicaltrials.gov)
    P1/2, N=346, Recruiting, Novartis Pharmaceuticals | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Erbitux (cetuximab) • Mekinist (trametinib) • Kisqali (ribociclib) • opnurasib (JDQ443)