More than 2/3 of newly diagnosed breast cancers are estrogen receptor (ER)-positive.  Inhibiting ER in these patients have been a long-pursued goal in order to treat these patients. Current standard of care (SOC) is the first-generation SERD fulvestrant. While fulvestrant is a strong ER inhibitor, it can only be administered through a painful monthly intramuscular injection due to low oral bioavailability and sub-optimal pharmacokinetic profile. Rising fulvestrant-resistant secondary mutations in ER coding gene (ESR1) are reported in ~40% patients. Once resistant, these patients have no effect treatment options. FWD1802 is a third-generation SERD that is 1) orally available, and 2) potent inhibitor of both wildtype and mutated ER. Therefore, FWD1802 has the potential to replace fulvestrant as new first-line SOC in the future. 


Program/TargetProg/Tgt
IndicationInd
DiscoveryDiscov
Lead
Optimization
Lead Opt
IND
Enabling
IND
Phase 1Ph 1
Phase 2Ph 2
CollaborationsCollab
FWD1802
ER+ Breast Cancer
FWD1802
(SERD)
ER+ Breast Cancer
Class I HDAC inhibition has been shown to dramatically enhance the efficacy of MEK inhibitors in Ras pathway driven melanomas by coordinately suppressing two DNA repair pathways. A potential clinical biomarker that predicts responsiveness has also been identified.