Therapy Detail

Therapy Name PD173074
Therapy Description

PD173074 is an ATP-competitive inhibitor of FGFR1, FGFR3, FGFR4, and KDR (VEGFR2), which may reduce proliferation and induce apoptosis in cancer cells (PMID: 9774334, PMID: 24126887, PMID: 14715624).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
PD173074 FGFR1 Inhibitor 21 FGFR3 Inhibitor 12 FGFR4 Inhibitor 7 VEGFR2 Inhibitor 34 PD173074 is an ATP-competitive inhibitor of FGFR1, FGFR3, FGFR4, and KDR (VEGFR2), which may reduce proliferation and induce apoptosis in cancer cells (PMID: 9774334, PMID: 24126887, PMID: 14715624).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR1 amp synovial sarcoma sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980). 27535980
FGFR2 L618M Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 L618M demonstrated a decreased response to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 E566G Advanced Solid Tumor resistant PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 E566G were resistant to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 M538I Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 M538I demonstrated a decreased response to treatment with PD173074 (PMID: 23908597). 23908597
AKT1 S266L FGFR1 amp lung cancer predicted - resistant PD173074 Preclinical - Cell culture Actionable In a preclinical study, lung cancer cells harboring FGFR1 amplification demonstrated resistance to increasing concentrations of PD173074 in culture and was subsequently, found to have acquired AKT1 S266L (PMID: 30140389). 30140389
FGFR3-TACC3 malignant glioma sensitive PD173074 Preclinical - Cell line xenograft Actionable In a preclinical study, PD173074 inhibited Fgfr3 kinase activity and growth in transformed astrocytes expressing the FGFR3-TACC3 fusion in culture and in cell line xenograft models (PMID: 22837387). 22837387
FGFR2 M536I Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 M536I demonstrated a decreased response to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 C383R FGFR2 N550K endometrial cancer resistant PD173074 Preclinical Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 C383R and expressing FGFR2 N550K demonstrated resistance when treated with PD173074 (PMID: 23908597). 23908597
FGFR1 positive uterus leiomyosarcoma decreased response PD173074 Preclinical - Cell culture Actionable In a preclinical study, uterine leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to PD173074 in culture (PMID: 27535980). 27535980
FGFR3 S249C FGFR3 over exp transitional cell carcinoma sensitive PD173074 Preclinical Actionable In a preclinical study, PD173074 inhibited growth of urothelial carcinoma (UC) cells expressing high levels of FGFR3 S249C, but had reduced efficacy against UC cells with low levels of FGFR3 S249C expression (PMID: 22869148). 22869148
FGFR2 over exp breast cancer sensitive PD173074 Preclinical Actionable In a preclinical study, PD173074 inhibited proliferation of breast cancer cells over expressing FGFR2 in culture (PMID: 22869148). 22869148
FGFR3 K650E FGFR3 over exp HRAS K117E multiple myeloma sensitive PD173074 Preclinical Actionable In a preclinical study, PD173074 inhibited Fgfr3 signaling, induced cell-cycle arrest, and decreased proliferation of multiple myeloma cells harboring HRAS H117E and over expression of FGFR3 K650E in culture (PMID: 22869148). 22869148
FGFR1-TACC1 malignant glioma sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited Fgfr1 kinase activity and cell growth in transformed cells expressing the FGFR1-TACC1 fusion in culture (PMID: 22837387). 22837387
FGFR2 N550K Advanced Solid Tumor resistant PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550K were resistant to PD173074 (PMID: 23908597). 23908597
FGFR2-BICC1 Advanced Solid Tumor sensitive PD173074 Preclinical Actionable In a preclinical study, treatment with PD173074 prevented transformation of cells expressing FGFR2-BICC1 in culture (PMID: 24122810). 24122810
FGFR1 over exp uterus leiomyosarcoma sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited survival of FGFR1 over expressing uterus leiomyosarcoma cells in culture (PMID: 27535980). 27535980
FGFR2 I548V Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 I548V demonstrated a decreased response to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 amp stomach cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, FGFR2-amplified gastric cancer cell lines demonstrated sensitivity to PD173074 in culture, with cell lines with high-level FGFR2 amplification displaying higher sensitivity compared to cell lines with low-level amplification (PMID: 27179038). 27179038
FGFR2 amp stomach cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited proliferation of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 26036639). 26036639
FGFR1 amp lung cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, lung cancer cells harboring FGFR1 amplification were sensitive to PD173074 treatment in culture, demonstrating inhibition of cell growth (PMID: 30140389). 30140389
FGFR3 wild-type FGFR3 dec exp HRAS G12V transitional cell carcinoma resistant PD173074 Preclinical Actionable In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to PD173074 in culture (PMID: 22869148). 22869148
FGFR2 amp myxoid liposarcoma sensitive PD173074 Preclinical Actionable In a preclinical study, PD173074 increased apoptosis, inhibited cell proliferation and migration of myxoid liposarcoma cell lines harboring FGFR2 amplification in culture (PMID: 26036639). 26036639
FGFR2 N550H Advanced Solid Tumor resistant PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550H were resistant to treatment with PD173074 (PMID: 23908597). 23908597
FGFR1 positive synovial sarcoma decreased response PD173074 Preclinical - Cell culture Actionable In a preclinical study, synovial sarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to PD173074 in culture (PMID: 27535980). 27535980
FGFR2 V565I Advanced Solid Tumor resistant PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 V565I were resistant to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2-AHCYL1 Advanced Solid Tumor sensitive PD173074 Preclinical Actionable In a preclinical study, treatment with PD173074 prevented transformation of cells expressing FGFR2-AHCYL1 in culture (PMID: 24122810). 24122810
FGFR3 G384D FGFR3 over exp multiple myeloma decreased response PD173074 Preclinical Actionable In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to PD173074 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). 22869148
FGFR1 positive leiomyosarcoma decreased response PD173074 Preclinical - Cell culture Actionable In a preclinical study, leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to PD173074 in culture (PMID: 27535980). 27535980
FGFR3-BAIAP2L1 urinary bladder cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3 Y373C FGFR3 over exp multiple myeloma sensitive PD173074 Preclinical Actionable In a preclinical study, PD173074 inhibited Fgfr3 signaling and decreased proliferation and survival of multiple myeloma cells over expressing FGFR3 Y373C in culture (PMID: 22869148). 22869148
FGFR2 N550S Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550S demonstrated a decreased response to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 K660E Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 K660E demonstrated a decreased response when treated with PD173074 (PMID: 23908597). 23908597
Clinical Trial Phase Therapies Title Recruitment Status