lns-8801

LNS‑8801 is an orally bioavailable and highly specific small molecule agonist of the G protein-coupled estrogen receptor (GPER), also known as GPR30. Developed by Linnaeus Therapeutics for oncology indications including melanoma and other solid tumors, it acts by activating GPER to rapidly and durably deplete c‑Myc protein levels in cancer cells. This leads to increased melanocytic differentiation, inhibition of proliferation and invasion in tumor cells, enhancement of immune recognition (including synergy with immune checkpoint inhibitors), induction of apoptosis via reactive oxygen species (ROS) production and endoplasmic reticulum stress pathways. Preclinical studies have shown potent antitumor activity across multiple tumor types with minimal toxicity to normal cells. Clinical trials have demonstrated safety and tolerability both as monotherapy and in combination with pembrolizumab[2][3][4][5][6].

Other names

Ethanone, 1-((3ar,4s,9bs)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)-, rel-881639–98–1Chembl569766Chembl-569766Chembl 569766