^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG CLASS:

    FAP inhibitor

    Related drugs:
    7d
    Translational Theranostics in Glioblastoma: FAPI-46 as a Precision Medicine Tool. (PubMed, J Nucl Med)
    [177Lu]Lu-FAPI-46 demonstrated lower therapeutic efficacy, as a monotherapy or in combination with temozolomide, than did [225Ac]Ac-FAPI-46. FAPI-46 demonstrates significant potential as a theranostic agent for glioblastoma in peripheral models. However, its inability to cross the blood-brain barrier in orthotopic models highlights the need for future studies to improve its clinical applicability.
    Journal
    |
    FAP (Fibroblast activation protein, alpha)
    |
    temozolomide • [177Lu]FAPI-46
    13d
    Evaluation of Fibrotic Disease Activity in Cardiopulmonary Disorders Using 18F-Fibroblast Activation Protein Inhibitor (18F-FAPI-74 PET/CT Imaging) (clinicaltrials.gov)
    P3, N=210, Not yet recruiting, National Heart, Lung, and Blood Institute (NHLBI)
    New P3 trial
    14d
    STARLYS: Phase 1 Open Label Trial of MST-0312 Alone and in Combination in Subjects With Solid Malignancies (clinicaltrials.gov)
    P1, N=157, Recruiting, Mestag Therapeutics Limited
    New P1 trial
    |
    Keytruda (pembrolizumab)
    14d
    BRAVO: Study of AZD2389 Safety, Tolerability, and Pharmacodynamics in Adults With Steatotic Liver Disease and Advanced Fibrosis (clinicaltrials.gov)
    P2, N=104, Recruiting, AstraZeneca
    New P2 trial
    |
    PRO-C3 (Pyrroline-5-carboxylate reductase)
    18d
    D7930C00003: A Phase 1 open-label positron emission tomography TRIAL to assess changes in liver uptake of [68Ga]Ga-FAPI-46 following oral administration of single doses of AZD2389 to patients with advanced liver fibrosis (PECHORA) (2024-517605-91-00)
    P1, N=12, Active, not recruiting, AstraZeneca AB | Recruiting --> Active, not recruiting
    Enrollment closed
    27d
    BXCL701-201: A Trial of BXCL701 and Pembrolizumab in Patients With mCRPC Either Small Cell Neuroendocrine Prostate Cancer or Adenocarcinoma Phenotype. (clinicaltrials.gov)
    P1/2, N=98, Completed, BioXcel Therapeutics Inc | Trial completion date: Dec 2024 --> Aug 2025
    Trial completion date
    |
    Keytruda (pembrolizumab) • talabostat (BXCL701)
    1m
    Phase 2 study of talabostat, a small molecule inhibitor of dipeptidyl peptidases (DPP), administered in combination with pembrolizumab in patients with small cell neuroendocrine prostate cancer. (PubMed, J Immunother Cancer)
    Talabostat plus pembrolizumab demonstrates preliminary anti-tumor activity in patients with relapsed SCNC. Further evaluation in a randomized study is warranted to assess the contribution of talabostat in this high-risk disease subset.
    P2 data • Journal • Tumor mutational burden • PD(L)-1 Biomarker
    |
    TMB (Tumor Mutational Burden) • DPP9 (Dipeptidyl Peptidase 9)
    |
    TMB-L
    |
    Keytruda (pembrolizumab) • talabostat (BXCL701)
    1m
    The evolving role of targeted radioligand therapy in small cell and non-small cell lung cancer: a systematic review. (PubMed, Explor Target Antitumor Ther)
    In NSCLC, fibroblast activation protein (FAP)-targeted agents such as [177Lu]Lu-FAP-2286 demonstrated partial metabolic responses, including a 44.4% response rate and 78% disease control in a mixed cohort...Early efficacy signals exist for strong somatostatin receptor (SSTR)-targeted therapy in SCLC and FAP-targeted therapy in NSCLC, but evidence remains limited. Prospective trials with standardized protocols and dosimetry are needed to define TRT's role in lung cancer treatment.
    Review • Journal
    |
    SSTR (Somatostatin Receptor)
    |
    lutetium Lu 177 rofapitide tetraxetan (AAA614)
    1m
    Safety and activity of RO7300490, a bispecific CD40 agonist targeted to fibroblast activation protein, in patients with advanced solid tumors: a single-arm, multicenter, first-in-human, phase 1 trial. (PubMed, Nat Cancer)
    In summary, treatment with a tumor-targeted CD40 agonist antibody is feasible, clinically manageable and induces immunomodulation of the tumor microenvironment. ClinicalTrials.gov registration: NCT04857138 .
    P1 data • Journal • First-in-human
    |
    LAMP3 (Lysosomal Associated Membrane Protein 3) • CD40 (CD40 Molecule)
    1m
    Tumor-localized CD40 agonism with MP0317, a FAP x CD40 DARPin, reprograms the tumor microenvironment in patients with advanced solid tumors: an open-label, nonrandomized, dose-escalation phase 1 study. (PubMed, Nat Cancer)
    Collectively, these data confirm a favorable safety profile for MP0317 and support further clinical evaluation in combination with complementary immunotherapies. ClinicalTrials.gov registration: NCT05098405 .
    P1 data • Journal • IO biomarker
    |
    IFNG (Interferon, gamma) • CD40 (CD40 Molecule)
    |
    MP0317
    1m
    Novel Covalent FAP-Targeted [68Ga]Ga-DOTA-mFS-KERERG-FAP-2286 for Improved Pharmacokinetics and Enhanced Tumor Uptake. (PubMed, Mol Pharm)
    The potential diagnostic value of [68Ga]Ga-DOTA-mFS-KERERG-FAP-2286 lies in its design as a derivative of the DOTA-FAP-2286 scaffold, incorporating a sulfur(VI) fluoride exchange (SuFEx)-based covalent warhead and a hydrophilic polypeptide. This modification is anticipated to alter the pharmacokinetic profile, leading to enhanced tumor uptake and retention, thereby improving clinical diagnostic accuracy.
    PK/PD data • Journal
    |
    FAP (Fibroblast activation protein, alpha)
    |
    lutetium Lu 177 rofapitide tetraxetan (AAA614)
    2ms
    A Phase 1a/1b Dose-Escalation and Expansion Study of [¹77Lu]Lu-FAP-2286 Radioligand Therapy in Combination with Dual Immune Checkpoint Blockade (Nivolumab and Ipilimumab) in Patients with Unresectable or Advanced Malignant Pleural Mesothelioma (MPM) (ACTRN12626000505303)
    P1, N=50, Not yet recruiting, South Metropolitan Health Service
    New P1 trial • Checkpoint inhibition
    |
    FAP (Fibroblast activation protein, alpha)
    |
    Opdivo (nivolumab) • Yervoy (ipilimumab) • lutetium Lu 177 rofapitide tetraxetan (AAA614)