Therapy Detail

Therapy Name rigosertib
Therapy Description

Estybon (rigosertib) inhibits polo-like kinase 1 (Plk1) and PI3K pathways, which induces selective G2/M arrest and apoptosis in tumor cells (PMID: 24777753).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Rigosertib Estybon ON 01910.Na|SyB L-1101 PI3K Inhibitor (Pan) 34 PLK1 Inhibitor 17 Estybon (rigosertib) inhibits polo-like kinase 1 (Plk1) and PI3K pathways, which induces selective G2/M arrest and apoptosis in tumor cells (PMID: 24777753).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown myelodysplastic syndrome no benefit rigosertib Phase III Actionable In a Phase III trial, Estybon (rigosertib) did not improve survival compared to best supportive care in patients with myelodysplastic syndrome (PMID: 26968357). 26968357
Unknown unknown Advanced Solid Tumor not applicable rigosertib Phase I Actionable In a Phase I study, Estybon (rigosertib) demonstrated both saftey and efficacy in patients with advanced solid tumors (PMID: 23841031). 23841031
KRAS G12D pancreatic cancer sensitive rigosertib Preclinical Actionable In a preclinical study, Estybon (rigosertib) inhibited tumorigenesis in transgenic animal model of pancreatic cancer driven by KRAS G12D (PMID: 27104980). 27104980
KRAS G13D colorectal cancer sensitive rigosertib Preclinical - Cell line xenograft Actionable In a preclinical study, Estybon (rigosertib) inhibited Mek/Erk signaling and tumor growth in cell line xenograft models of colorectal cancer harboring KRAS G13D (PMID: 27104980). 27104980
KRAS G12S lung cancer sensitive rigosertib Preclinical - Cell line xenograft Actionable In a preclinical study, Estybon (rigosertib) inhibited Mek/Erk signaling and tumor growth in cell line xenograft models of lung cancer harboring KRAS G12S (PMID: 27104980). 27104980
PTEN loss head and neck squamous cell carcinoma predicted - sensitive rigosertib Phase I Actionable In a Phase I trial in patients with advanced solid tumors, Estybon (rigosertib) treatment resulted in responses in 2 patients with head and neck squamous cell carcinoma (1 complete response and 1 partial response), 1 harboring PIK3CA amplification and the other harboring PTEN loss (Cancer Res April 15 2013 (73) (8 Supplement) LB-198). detail...
HRAS G12V Advanced Solid Tumor sensitive rigosertib Preclinical - Cell culture Actionable In a preclinical study, Estybon (rigosertib) inhibited oncogenic transformation in fibroblast cells over-expressing HRAS G12V in culture (PMID: 27104980). 27104980
Clinical Trial Phase Therapies Title Recruitment Status
NCT01928537 Phase III rigosertib Efficacy and Safety of IV Rigosertib in MDS Patients With Excess Blasts Progressing After Azacitidine or Decitabine Active, not recruiting
NCT02562443 Phase III rigosertib Controlled Study of Rigosertib Versus Physician's Choice of Treatment in MDS Patients After Failure of an HMA (INSPIRE) Recruiting
NCT01584531 Phase II rigosertib Efficacy and Safety of Oral Rigosertib in Transfusion-dependent, Low or Int-1 or Trisomy 8 Int-2 Myelodysplastic Syndrome Completed
NCT02107235 Phase I Cisplatin rigosertib Platinum-based Chemoradiotherapy and Rigosertib in Head and Neck Cancer Completed