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    DRUG CLASS:

    PDGFR α-β inhibitor

    Related drugs:
    5ms
    Open-label Extension Study of GB002 in Adult Subjects With Pulmonary Arterial Hypertension (PAH) (clinicaltrials.gov)
    P2, N=74, Active, not recruiting, GB002, Inc., a wholly owned subsidiary of Gossamer Bio, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    1year
    An open-lable phase Ib/II study, Lucitanib combined with Toripalimab in the treatment of advanced recurrent or metastatic solid tumors (ChiCTR2400087935)
    P1/2, N=180, Completed, Sun Yat-sen University Cancer Center; Haihe Biopharma Co.,Ltd.
    New P1/2 trial • Metastases
    |
    Loqtorzi (toripalimab-tpzi) • lucitanib (E 3810)
    over1year
    Fibroblast growth factor receptor signaling in estrogen receptor-positive breast cancer: mechanisms and role in endocrine resistance. (PubMed, Front Oncol)
    Current clinical trials, including those evaluating FGFR inhibitors like erdafitinib, lucitanib, and dovitinib, have demonstrated mixed outcomes, underscoring the complexity of FGFR signaling in breast cancer. In conclusion, targeting FGFR signaling in ER+ breast cancer presents both challenges and opportunities. A deeper understanding of the molecular mechanisms and resistance pathways is crucial for the successful integration of FGFR inhibitors into clinical practice, aiming to improve outcomes for patients with endocrine-resistant breast cancer.
    Review • Journal
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    ER (Estrogen receptor) • FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • FGFR4 (Fibroblast growth factor receptor 4) • NSD3 (Nuclear Receptor Binding SET Domain Protein 3) • EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1)
    |
    Balversa (erdafitinib) • dovitinib (TKI258) • lucitanib (E 3810)
    over1year
    Open-label Extension Study of GB002 in Adult Subjects With Pulmonary Arterial Hypertension (PAH) (clinicaltrials.gov)
    P2, N=100, Recruiting, GB002, Inc., a wholly owned subsidiary of Gossamer Bio, Inc. | Trial completion date: Jul 2025 --> Dec 2027 | Trial primary completion date: Jul 2025 --> Dec 2027
    Trial completion date • Trial primary completion date
    over2years
    REGISTRI: Single Agent Regorafenib in First-line for Metastatic/Unresectable KIT/PDGFR Wild Type GIST (clinicaltrials.gov)
    P2, N=15, Completed, Grupo Espanol de Investigacion en Sarcomas | Recruiting --> Completed | N=39 --> 15
    Trial completion • Enrollment change • Metastases
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    KIT (KIT proto-oncogene, receptor tyrosine kinase)
    |
    KIT mutation • KIT exon 11 mutation • KIT exon 13 mutation • KIT exon 17 mutation • KIT wild-type • PDGFR wild-type
    |
    Stivarga (regorafenib)
    over2years
    STREAM: Regorafenib Monotherapy as Second-line Treatment of Patients With RAS-mutant Advanced Colorectal Cancer (clinicaltrials.gov)
    P2, N=46, Active, not recruiting, National Cancer Institute, Naples | Trial completion date: Nov 2022 --> Nov 2024 | Trial primary completion date: Nov 2021 --> Nov 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    RAS (Rat Sarcoma Virus)
    |
    RAS mutation
    |
    Stivarga (regorafenib)
    over2years
    Regorafenib and PD-1 Antibody in Combination With Radiotherapy for pMMR/MSS Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=28, Recruiting, Sun Yat-sen University | Unknown status --> Recruiting | N=43 --> 28 | Trial completion date: Jul 2020 --> Jul 2023 | Trial primary completion date: Jul 2020 --> Feb 2023
    Enrollment open • Enrollment change • Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS wild-type • RAS wild-type
    |
    Stivarga (regorafenib)
    over2years
    An Exploration of Trifluridine/Tipiracil Monotherapy and in Combination With Bevacizumab or Immune Checkpoint Inhibitors for Patients With Metastatic Colorectal Cancer: A Real-World Study. (PubMed, Clin Colorectal Cancer)
    In real-world clinical setting, TAS-102 showed consistent clinical efficacy and manageable safety with previous prospective clinical studies. Compared with monotherapy and TAS-102 plus ICIs, TAS-102 plus bevacizumab demonstrated better clinical efficacy for metastatic colorectal cancer.
    Journal • Combination therapy • Checkpoint inhibition • Real-world evidence • Real-world • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Avastin (bevacizumab) • Stivarga (regorafenib) • Fruzaqla (fruquintinib) • Lonsurf (trifluridine/tipiracil)
    over2years
    Circulating Tumor DNA Dynamics and Treatment Outcome of Regorafenib in Metastatic Colorectal Cancer. (PubMed, Cancer Res Treat)
    VAF of the majority of the ctDNA mutations increased at the time of disease progression, and VAF of BRAF increased markedly. Reduction in ctDNA burden as estimated by sum (VAF) could be used to predict treatment outcome of regorafenib.
    Journal • Circulating tumor DNA • Metastases
    |
    BRAF (B-raf proto-oncogene) • TP53 (Tumor protein P53) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • TCF7L2 (Transcription Factor 7 Like 2)
    |
    TP53 mutation
    |
    Stivarga (regorafenib)
    over2years
    Using a combination of fruquintinib, raltitrexed, and S-1 as a third-line treatment for metastatic colorectal cancer with co-existence of Hodgkin lymphoma: a case report. (PubMed, J Gastrointest Oncol)
    Fruquintinib, regorafenib, trifluridine/tipiracil (TAS-102), panitumumab and cetuximab combined with single-agent chemotherapy regimens are currently recommended as third-line therapies for patients exhibiting disease progression...The mFOLFOX6 regimen was administered...Liver metastases (intestinal-type adenocarcinoma) were detected in November 2018, and second-line therapy with the FOLFIRI regimen was initiated in January 2019...Third-line therapy with fruquintinib, raltitrexed, and S-1 achieved a PR that permitted surgical resection and enabled a relatively long progression-free survival. The findings suggest that the three agents regimen might be clinically effective as late-line therapy for mCRC.
    Clinical • Journal • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation • RAS wild-type
    |
    Erbitux (cetuximab) • 5-fluorouracil • Vectibix (panitumumab) • Stivarga (regorafenib) • oxaliplatin • irinotecan • Fruzaqla (fruquintinib) • Lonsurf (trifluridine/tipiracil) • leucovorin calcium • Teysuno (gimeracil/oteracil/tegafur) • Tomudex (raltitrexed)
    over2years
    A Real-World Comparison of Regorafenib and Trifluridine/Tipiracil in Refractory Metastatic Colorectal Cancer in the United States. (PubMed, J Natl Compr Canc Netw)
    This analysis of real-world data found that OS was similar for patients with mCRC who were treated with TAS-102 compared with regorafenib. Median OS with both agents in a real-world setting was similar to that shown in the clinical trials that led to their approvals. A prospective trial comparing TAS-102 and regorafenib would unlikely change current management of patients with refractory mCRC.
    Journal • Real-world evidence • Real-world • Metastases
    |
    MSI (Microsatellite instability)
    |
    Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)