Pipeline & Targets
- FGFR3 (TYRA-300) *First patient dosed
- FGFR1/2/3 (TYRA-200)
- FGFR3 (ACH)
Indication: Bladder and solid tumors
FGFR3 mutation incidence: The incidence of activating FGFR3 mutations in bladder cancer has been estimated to be as high as 75% in non-muscle invasive bladder cancer (NMIBC) and up to 20% in muscle invasive bladder cancer (MIBC).
TYRA-200 is an FGFR1/2/3 inhibitor with potency against FGFR2 fusions, molecular brake mutations and gatekeeper resistance that TYRA is developing initially in intrahepatic cholangiocarcinoma.
Resistance to currently approved FGFR inhibitors for FGFR2 fusion positive intrahepatic cholangiocarcinoma (ICC) has been reported due to acquired mutations in FGFR2 , including the gatekeeper and residues comprising the molecular brake.
Indication: Bile duct and solid tumors
FGFR2 mutation incidence: Approximately 15-20% of patients with ICC have genetic alterations in FGFR2, which are primarily gene fusions and activating mutations.
FGFR3 (Skeletal dysplasias including ACH)
Our drug discovery efforts are driven by structural insights into the FGFR3 selectivity we have observed with TYRA-300. The FGFR3 (ACH) program is in the discovery stage.
FGFR3 mutation incidence: Approximately 80% of cases of achondroplasia arise through spontaneous mutation of FGFR3.
Our drug discovery efforts are driven by our deep understanding of FGFR family structure and the FGFR4 protein specifically. The FGFR4 program is in discovery stage.
Indication: Liver and solid tumors
FGFR4 mutation incidence: FGFR4 gene alterations such as activating point mutations and fusions have been identified in rare populations such as pediatric rhabdomyosarcoma and a variety of other solid tumors.
Our drug discovery efforts are driven by our ability to gain molecular-level detail and insights from internally derived co-crystal structures of current RET inhibitors bound to receptor tyrosine kinases. The RET program is in the discovery stage.
Indication: Lung and thyroid cancer
RET mutation incidence: In non-small cell lung cancer (NSCLC), 1 to 2% of patients who are negative for mutations or rearrangements in other common oncogenic drivers have RET fusions. In papillary thyroid carcinoma (PTC), the most common form of thyroid cancer, an estimated 35% of cases in North America and up to 65% of cases in other geographies are associated with RET fusions. In sporadic medullary thyroid carcinoma, or MTC, approximately half of patients have activating mutations in RET.