^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG:

    cirtuvivint (SM08502)

    i
    Other names: SM08502, SM 08502, SM-08502
    Company:
    Biosplice Therap
    Drug class:
    pan-CLK inhibitor, DYRK inhib
    Related drugs:
    3d
    SM08502-Mediated β-Catenin Repression Synergizes with Olaparib to Inhibit Tumor Progression. (PubMed, Cancer Res Commun)
    Overcoming PARPi resistance will provide patients with therapeutic options. The study shows, in the context of resistant disease, the potential of targeting CDC-like kinase/dual-specificity tyrosine phosphorylation-regulated kinase alone and in combination with PARP inhibitors.
    Journal • BRCA Biomarker • PARP Biomarker • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency) • PD-1 (Programmed cell death 1) • CTNNB1 (Catenin (cadherin-associated protein), beta 1)
    |
    PD-L1 expression
    |
    Lynparza (olaparib) • cirtuvivint (SM08502)
    3ms
    Cirtuvivint/Olaparib in Breast Cancer Susceptibility Gene/Homologous Recombination Deficiency Platinum Resistant Ovarian Cancer (clinicaltrials.gov)
    P1, N=50, Recruiting, University of Colorado, Denver | Not yet recruiting --> Recruiting
    Enrollment open • Platinum resistant
    |
    BRCA (Breast cancer early onset)
    |
    Lynparza (olaparib) • cirtuvivint (SM08502)
    3ms
    RNA processing kinase inhibitors and epigenetic inhibitors in combination with oncology drugs or investigational agents in multi-cell type patient-derived tumor cell line spheroids. (PubMed, Cancer Chemother Pharmacol)
    These findings may provide guidance for development of clinical trial combination regimens including cirtuvivint, CC-671 or iadademstat. Full data sets are available on PubChem.
    Preclinical • Journal • IO biomarker
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D
    |
    MRTX1133 • eltanexor (KPT-8602) • iadademstat (ORY-1001) • cirtuvivint (SM08502)
    3ms
    Small Cell Lung Cancer Irinotecan and CDC2-like Kinase Inhibition Trial (SLICK Trial) (clinicaltrials.gov)
    P1/2, N=42, Not yet recruiting, Washington University School of Medicine
    New P1/2 trial
    |
    irinotecan • cirtuvivint (SM08502)
    6ms
    RNA processing kinase inhibitors and epigenetic inhibitors in combination with oncology drugs or investigational agents in multi-cell type patient-derived tumor cell line spheroids. (PubMed, Res Sq)
    We investigated the activity of two CLK inhibitors, cirtuvivint and CC-671, and the LSD1 inhibitor iadademstat alone and in combination with anticancer drugs or investigational agents...These agents included the XPO1 inhibitor, eltanexor, and the KRAS G12D specific inhibitor MRTX-1133 which had activity in tumor lines harboring the KRAS G12D mutation. LSD1 inhibition was effective with ubiquitin proteasome pathway inhibitors. The full data sets are available on PubChem.
    Preclinical • Journal • IO biomarker
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12D
    |
    MRTX1133 • eltanexor (KPT-8602) • iadademstat (ORY-1001) • cirtuvivint (SM08502)
    9ms
    Cirtuvivint/Olaparib in Breast Cancer Susceptibility Gene/homologous Recombination Deficiency Platinum Resistant Ovarian Cancer (clinicaltrials.gov)
    P1, N=50, Not yet recruiting, University of Colorado, Denver
    New P1 trial
    |
    BRCA (Breast cancer early onset)
    |
    Lynparza (olaparib) • cirtuvivint (SM08502)
    1year
    Targeting the CLK2/SRSF9 splicing axis in prostate cancer leads to decreased ARV7 expression. (PubMed, Mol Oncol)
    Inhibition of the Cdc2-like kinase (CLK) family by the small molecules cirtuvivint or lorecivivint results in the decreased expression of ARV7. Both inhibitors show potent anti-proliferative effects in enzalutamide-treated or -naive PC models. Thus, targeting aberrant alternative splicing at the 3'UTR of ARV7 by disturbing the CLK2/SRSF9 axis might be a valuable therapeutic approach in late stage, ARSI-resistant PC.
    Journal
    |
    AR (Androgen receptor) • ARSI (Arylsulfatase Family Member I) • CDK1 (Cyclin-dependent kinase 1) • CLK2 (CDC Like Kinase 2) • SRSF9 (Serine And Arginine Rich Splicing Factor 9)
    |
    AR splice variant 7 • AR-V7 expression
    |
    Xtandi (enzalutamide) • lorecivivint (SM04690) • cirtuvivint (SM08502)
    over1year
    A Study Evaluating the Safety, Pharmacokinetics, and Preliminary Efficacy of Orally Administered SM08502 Combined With Hormonal Therapy or Chemotherapy in Subjects With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=30, Terminated, Biosplice Therapeutics, Inc. | Phase classification: P1b --> P1 | Active, not recruiting --> Terminated; Study was terminated due business reasons by Sponsor.
    Phase classification • Trial termination • Metastases
    |
    ALK (Anaplastic lymphoma kinase) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    docetaxel • 5-fluorouracil • Vectibix (panitumumab) • abiraterone acetate • irinotecan • prednisone • leucovorin calcium • cirtuvivint (SM08502)
    over1year
    A Study Evaluating the Safety and Pharmacokinetics of Orally Administered SM08502 in Subjects With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=82, Terminated, Biosplice Therapeutics, Inc. | Active, not recruiting --> Terminated; Study was terminated due business reasons by Sponsor.
    Trial termination • Metastases
    |
    cirtuvivint (SM08502)
    3years
    A Study Evaluating the Safety, Pharmacokinetics, and Preliminary Efficacy of Orally Administered SM08502 Combined With Hormonal Therapy or Chemotherapy in Subjects With Advanced Solid Tumors (clinicaltrials.gov)
    P1b, N=30, Active, not recruiting, Biosplice Therapeutics, Inc. | Recruiting --> Active, not recruiting | N=150 --> 30 | Trial primary completion date: Jul 2026 --> Jul 2024
    Enrollment closed • Enrollment change • Trial primary completion date • Metastases
    |
    ALK (Anaplastic lymphoma kinase) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    EGFR mutation
    |
    docetaxel • 5-fluorouracil • Vectibix (panitumumab) • abiraterone acetate • irinotecan • prednisone • leucovorin calcium • cirtuvivint (SM08502)