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Therapy Name | PD173074 |
Synonyms | |
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, PMID: 30544798). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
PD173074 | PD-173074|PD 173074 | FGFR1 Inhibitor 28 FGFR3 Inhibitor 19 FGFR4 Inhibitor 9 VEGFR2 Inhibitor 37 | 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, PMID: 30544798). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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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 |
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 |
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 |
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 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 K310R FGFR2 N550K | endometrial cancer | sensitive | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, PD173074 treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 N550K and K310R in culture (PMID: 30537101). | 30537101 |
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 |
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 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 |
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 K652E | urinary bladder cancer | resistant | PD173074 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, bladder cancer cells harboring FGFR3 K652E were resistant to PD173074 in culture and in cell line xenograft models (PMID: 23558953). | 23558953 |
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 |
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 |
FGFR3 dec exp FGFR3 wild-type 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 N550K | endometrial cancer | predicted - sensitive | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, PD173074 treatment induced cell death in an endometrial cancer cell line harboring FGFR2 N550K in culture (PMID: 30537101). | 30537101 |
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 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 |
FGFR2 amp | stomach cancer | sensitive | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, PD173074 inhibited growth of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 30045926). | 30045926 |
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 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 |
FGFR3 S249C | urinary bladder cancer | resistant | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, bladder cancer cells harboring FGFR3 S249C were resistant to PD173074 in culture (PMID: 23558953). | 23558953 |
FGFR3 K650E FGFR3 over exp HRAS K117E | multiple myeloma | sensitive | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, PD173074 inhibited Fgfr3 signaling, induced cell cycle arrest, and decreased proliferation of multiple myeloma cells harboring HRAS K117E and overexpression of FGFR3 K650E in culture (PMID: 22869148). | 22869148 |
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 |
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 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 C383R | endometrial cancer | sensitive | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, PD173074 treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 C383R in culture (PMID: 30537101). | 30537101 |
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 N550K | Advanced Solid Tumor | resistant | PD173074 | Preclinical | Actionable | In a preclinical study, transformed cells expressing FGFR2 N550K were resistant to PD173074 (PMID: 23908597). | 23908597 |
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 |
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 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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