Green3Bio – Developing A SIK inhibitor (GRN-300) For Ovarian cancer

GRN-300 is a first-in-class clinical agent – FDA cleared to initiate Phase 1 in Ovarian Cancer Patients at MD Anderson Cancer Center

  • Ovarian cancer is one of the leading forms of cancer; affecting an estimated 185,000 patients in 2020
  • The 5-year survival rate for all stages is 47%
  • GRN-300 is a first-in-class SIK inhibitor for Ovarian cancer and other cancers
  • In animal models GRN-300 is synergistic with paclitaxel
  • FDA cleared GRN-300 to initiate Phase 1 in Ovarian cancer at MD Anderson Cancer Center (2020 start)

GRN-300 is an orally bioavailable small-molecule inhibitor of the salt-inducible kinase 2 and 3 (SIK2, SIK3). The SIK2 kinase is overexpressed in 30% of ovarian cancer specimens suggesting a clinical mechanism of treating ovarian cancer by blocking SIK2 kinase activity. SIK2 and SIK3 are prevalent in several other tumor types, including prostate cancer, breast cancer, diffuse large B-cell lymphoma, and melanoma.

Higher levels of expression of SIK2 have been shown to be significantly correlated with poor progression-free survival in patients with high-grade serous ovarian cancers. GRN-300 demonstrated activity in animal models as a single agent for the treatment of ovarian carcinoma and in combination with paclitaxel.

Read about studies of our related compound in ovarian cancer models here.