Tyra Biosciences Pipeline & Targets

We have built a robust pipeline that leverages our rapid structure-based design process and unique insights into kinase family structures gained through internally derived co-crystal structures. Our initial focus is on improving small molecule drug discovery and development in targeted oncology and genetically defined conditions.

Tyra Pipeline
  • FGFR3 (Dabogratinib ACH)    
  • FGFR3 (Dabogratinib NMIBC)
  • FGFR3 (Dabogratinib LG-UTUC)  *IND Cleared
  • FGFR3 (Dabogratinib mUC) 
  • FGFR4/3 (TYRA-430)   
  • FGFR1/2/3 (TYRA-200) 
FGFR3 (Skeletal dysplasia including ACH)

We are developing dabogratinib with the goal of addressing long-term complications and improving quality of life in affected individuals with skeletal dysplasia including achondroplasia, a genetic condition caused by a mutation in the FGFR3 gene.

Our drug discovery efforts are driven by structural insights informed by hundreds of internally solved FGFR crystal structures. The dabogratinib (ACH) program is in Phase 2, the study is called BEACH301.

Targeted Indication: Achondroplasia

FGFR3 mutation incidence: Greater than 99% of achondroplasia arise through spontaneous mutation of FGFR3.

FGFR3 (Dabogratinib Onc, formerly TYRA-300)

Our lead product candidate, dabogratinib, is an investigational inhibitor of FGFR3 that is designed to be potent and selective in an effort to address two critical limitations of current approved and investigational FGFR inhibitors: activity in the presence of treatment-emergent resistance mutations such as the V555 gatekeeper mutation, and selectivity for FGFR3 over FGFR1 and other FGFR isoforms with the goal to avoid off-target side effects.

Targeted Indications: 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 approximately 85% in LG-UTUC.

FGFR4/3 (TYRA-430)

TYRA-430 is an investigational, FGFR4/3-biased inhibitor for FGF19+/FGFR4-driven cancers. The Phase 1 study is a multicenter, open-label, first-in-human study of TYRA-430 in advanced hepatocellular carcinoma (HCC) and other solid tumors with activating FGF/FGFR pathway aberrations (SURF431).

FGFR1/2/3 (TYRA-200)

TYRA-200 is an investigational, oral, FGFR1/2/3 inhibitor that has demonstrated potency in vitro against activating FGFR2 gene alterations and resistance mutations, currently in development for the treatment of cancer. TYRA-200 is being evaluated in a multi-center, open label Phase 1 clinical study, SURF201 (Study in PrevioUsly treated and Resistant FGFR2+ Cholangiocarcinoma and Other Advanced Solid Tumors). SURF201 (NCT06160752) was designed to determine the MTD and the RP2D of TYRA-200, as well as to evaluate the preliminary antitumor activity of TYRA-200. SURF201 is currently enrolling adults with advanced/metastatic intrahepatic cholangiocarcinoma and other advanced solid tumors with activating alterations in FGFR2.

Targeted Indications: 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.