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    DRUG CLASS:

    FAP inhibitor

    Related drugs:
    2d
    A Phase 1 Study of 177Lu-IM-3050 in Participants With Advanced Cancer (clinicaltrials.gov)
    P1, N=105, Recruiting, Immunome, Inc. | Not yet recruiting --> Recruiting
    Enrollment open • First-in-human
    8d
    18F-Fibroblast Activation Protein Inhibitor (18F-FAPI-74) in Tuberculosis Patients (clinicaltrials.gov)
    P=N/A, N=30, Recruiting, Children's Hospital Medical Center, Cincinnati | Not yet recruiting --> Recruiting
    Enrollment open
    14d
    PET Imaging of Solid Tumors by a Novel Tracer, 68Ga-FAPI (clinicaltrials.gov)
    P1, N=410, Recruiting, Karolinska University Hospital | Not yet recruiting --> Recruiting
    Enrollment open
    1m
    Initial Clinical Experience with [177Lu]Lu-RTX-2358 Radiopharmaceutical Therapy Targeting Fibroblast Activation Protein: Biodistribution, Pharmacokinetics, and Dosimetry. (PubMed, J Nucl Med)
    [177Lu]Lu-RTX-2358 demonstrated a manageable safety profile in a series of patients who were heavily pretreated for their disease. Given a promising therapeutic index as a result of prolonged retention in tumors and clearance from normal organs, further clinical evaluation is warranted.
    PK/PD data • Journal
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    FAP (Fibroblast activation protein, alpha)
    1m
    A study to investigate safety and anti-tumour activity of a Fibroblast Activation Protein (FAP)-targeting radiotracer (177Lu-FO-004) & Safety and Tolerability of a FAP imaging agent (68Ga-3BP-3940) in patients with advanced cancer. (ACTRN12625000361404)
    P1, N=56, Recruiting, 3B Pharmaceuticals GmbH | Not yet recruiting --> Recruiting
    Enrollment open • Trial initiation date
    1m
    Fibroblast Activation Protein Inhibitor Theranostics in Sarcoma: Current Evidence and Future Directions. (PubMed, Clin Nucl Med)
    Various FAPI radiotracers, including FAPI-04, FAPI-46, and FAP-2286, offer unique pharmacokinetic properties...However, challenges remain, including FAP expression heterogeneity and the need for optimized treatment protocols. The aim of this review is to provide a comprehensive overview of the current evidence and future directions of FAPI-based theranostics in sarcoma management, highlighting its potential to improve patient outcomes.
    Journal
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    FAP (Fibroblast activation protein, alpha)
    |
    lutetium Lu 177 rofapitide tetraxetan (AAA614)
    2ms
    CAAA614A12101: LuMIERE: A Phase 1/2, Multicenter, Open label, Non randomized Study to Investigate Safety and Tolerability, Pharmacokinetics, Dosimetry, and Preliminary Activity of [177Lu]Lu-FAP-2286 in Participants with an Advanced Solid Tumor (2023-508995-12-01)
    P1/2, N=36, Recruiting, Novartis Pharma AG
    New P1/2 trial
    |
    HER-2 positive • HR positive • HER-2 negative • EGFR positive • HR positive + HER-2 negative
    |
    5-fluorouracil • albumin-bound paclitaxel • oxaliplatin • irinotecan • leucovorin calcium • lutetium Lu 177 rofapitide tetraxetan (AAA614)
    2ms
    Combination with Immunocytokines Enhances the Anticancer Activity of Small Molecule Drug Conjugates and Radioligand Therapeutics Targeting Fibroblast Activation Protein. (PubMed, Mol Pharm)
    A therapy experiment in immunocompetent mice bearing low FAP-expressing tumors showed that the combination with L19-hIL2 potentiated the antitumoral activity of 177Lu-OncoFAP-23 and OncoFAP-GlyPro-MMAE. These results provided the motivation for the clinical development of these combinations for treating FAP-positive solid tumors.
    Journal
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    FAP (Fibroblast activation protein, alpha)
    2ms
    A Study to Test BI 765179 Alone and in Combination With Ezabenlimab in Patients With Advanced Cancer (Solid Tumors) and BI 765179 in Combination With Pembrolizumab in Patients With Advanced Head and Neck Cancer (clinicaltrials.gov)
    P1, N=149, Active, not recruiting, Boehringer Ingelheim | Recruiting --> Active, not recruiting | Trial completion date: May 2028 --> Feb 2028
    Enrollment closed • Trial completion date
    |
    Keytruda (pembrolizumab) • ezabenlimab (BI 754091) • BI 765179
    2ms
    FAPI-PETCD: 68Ga-FAPI-46 PET/CT for Assessing Small Bowel Fibrostenosis in Crohn's Disease (clinicaltrials.gov)
    P1, N=45, Recruiting, Mayo Clinic | Not yet recruiting --> Recruiting
    Enrollment open
    2ms
    Safety Trial of 68Ga/177Lu-NRT6020 in FAP-Positive Advanced Solid Tumor Patients (clinicaltrials.gov)
    P1, N=132, Recruiting, Chengdu New Radiomedicine Technology Co. LTD. | Not yet recruiting --> Recruiting | Initiation date: Jul 2025 --> Nov 2025
    Enrollment open • Trial initiation date
    2ms
    Radiolabelled FAPI Radiotracers in Oncology: A Comprehensive Review of Current Diagnostic and Emerging Therapeutic Applications. (PubMed, Pharmaceuticals (Basel))
    Therapeutic evidence shows encouraging tumour retention and safety profiles for agents such as [177Lu]Lu-FAP-2286 and [90Y]Y-FAPI-46, while α-emitting radiotracers (e.g., [225Ac]Ac-FAPI-04) demonstrate potent antitumor effects in preclinical models...Nonetheless, clinical evidence remains in its early stages, and substantial questions persist regarding dosimetry, intertumoral variability in FAP expression, and optimal ligand selection for therapy. Continued development of next-generation FAPI constructs, along with well-designed prospective trials, will be crucial in defining the future role of FAPI-based theranostics in oncology.
    Review • Journal
    |
    FAP (Fibroblast activation protein, alpha)
    |
    lutetium Lu 177 rofapitide tetraxetan (AAA614)