fibroblast activation protein (fap)

FAPI-2 is a specific inhibitor of fibroblast-activated protein based on the radiotracer FAP labeling. It has anticancer activity and can be used in the study of pancreatic cancer.

The FAP-targeting peptide for FXX489 constitutes the peptide moiety of FXX489, suitable for biochemical assays and drug synthesis studies. FXX489 is a fibroblast activation protein (FAP)-targeting ligand employed in radioligand therapy (RLT) for multiple cancers.

FAPI-4 FAPI-4 is a fibroblast activating protein (FAP) inhibitor, a FAPI ligand, which shows strong liver uptake in PET imaging of primary liver cancer hepatocellular carcinoma (HCC) and is commonly used in PET imaging for the study of cancer.

FAPI-mFS, an irreversible fibroblast activation protein (FAP) inhibitor, enhances uptake and retention in cancer cells through its covalent binding properties with FAP. When labeled with radioactive 68Ga or 177Lu, FAPI-mFS can be utilized for cancer imaging and therapy.

3BP-3580 is an inhibitor of fibroblast activation protein (FAP) with a pIC50 value of 8.6, utilized in cancer research.

QI-18 is a fibroblast activation protein (FAP) inhibitor with an IC50 value of 0.50 nM, offering a 6.5-fold increase in activity compared to UAMC-1110 (IC50 3.25 nM). It can be utilized in the synthesis of highly tumor-selective and high-dose radiotracers for the diagnosis and treatment of tumors.

FAP-targeting peptide-PEG2 conjugate (Example A1) is the polypeptide and linker conjugate component of Unlabeled FXX489. Unlabeled FXX489 serves as a ligand targeting fibroblast activation protein (FAP).

DOTAGA-FAP-2286-ALB is a derivative of Rofapitide tetraxetan. It functions as a selective inhibitor of fibroblast activation protein (FAP) with an IC50 value of 67.5 nM. By interacting with albumin, DOTAGA-FAP-2286-ALB enhances tumor retention, prolongs circulation time in the bloodstream, and improves the stability of radiometal complexes [such as 111In and 225Ac]. This compound shows promise for use in targeted radionuclide therapy (TRT) research for FAP-positive solid tumors.

PNT6555 acts as an inhibitor of fibroblast activation protein-α (FAP). It possesses anti-tumor properties and is applicable for imaging FAP-positive tumors.

FAP-IN-4 (Comp 10) is an inhibitor of fibroblast activation protein (FAP) and serves as a targeted FAP-specific radiotracer for PET imaging labeled with 18F. It is applicable in tumor research.

ARI-3099 inhibits fibroblast activation protein, alpha (FAP).

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630/624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

FAPI-46 is a radiotracer for fibroblast activation protein (FAP), belonging to the class of FAP inhibitors (iFAP), and can be conjugated with labels such as 68Ga or 177Lu to serve as a tracer for FAP tumours in positron emission tomography (PET).

OncoFAP acetate is the highest-affinity small organic fibroblast activation protein (FAP) ligand reported to date, exhibiting a dissociation constant of 680 pM as measured by fluorescence polarization. OncoFAP derivatives, when administered intravenously in both fluorescent and radiolabeled forms, selectively accumulate in FAP-positive tumors while sparing normal tissues, enabling OncoFAP acetate to serve as modular components for targeted therapeutic delivery of radionuclides, CAR-T cells, or cytotoxic agents in oncology studies.

BR103354 is a novel fibroblast activation protein (FAP) inhibitor with anti-diabetic and anti-steatotic effects. BR103354 inhibited FAP with an IC50 value of 14 nM, showing high selectivity against dipeptidyl peptidase (DPP)-related enzymes and prolyl oligopeptidase (PREP). BR103354 exhibited good pharmacokinetic properties as evidenced by oral bioavailability of 48.4% and minimal hERG inhibition. Single co-administration of BR103354 with hFGF21 reduced nonfasting blood glucose concentrations, in association with increased intact form of hFGF21 in ob/ob mice. BR103354 acts as an effective FAP inhibitor in vitro and in vivo, thereby demonstrating its potential application as an anti-diabetic and anti-NASH agent.

NOTA-FAPI is a fibroblast activation protein (FAP) inhibitor and structural analogue of FAPI-4. NOTA-FAPI-4 serves as a diagnostic and therapeutic tool for diseases characterized by FAP overexpression, including its application as a positron emission tomography (PET) tracer for noninvasive imaging of FAP-associated pathological conditions and monitoring of therapeutic responses.

Suc-Gly-Pro-AMC, a fibroblast activation protein (FAP)-specific substrate, facilitates the examination of FAP activity [1].

FSDD0I, an albumin-binding fibroblast activation protein (FAP) ligand, can be labeled with 68Ga and 177Lu for use in single photon emission computed tomography (SPECT) imaging [1].

FSDD1I, an albumin-binding fibroblast activation protein (FAP) ligand, can be tagged with 68 Ga and 177 Lu for use in single photon emission computed tomography (SPECT) imaging [1].

FSDD3I, an albumin-binding fibroblast activation protein (FAP) ligand, can be tagged with isotopes 68Ga and 177Lu for use in single photon emission computed tomography (SPECT) imaging [1].

Rofapitide tetraxetan (FAP-2286) is a high-affinity, selective inhibitor of fibroblast activating protein (FAP) and a DOTA-pseudopeptide with an IC₅₀ of 1.3–2.2 nM. FAP-2286 targets the tumour microenvironment and can be radiolabelled (e.g., with ⁶⁸Ga) for use in positron emission tomography (PET) imaging.

FAP-2286 acetate, a conjugate of a fibroblast activation protein (FAP)-binding peptide, exhibits antitumor activity [1]. It can be labeled with radionuclides for diagnostic purposes.

FAP-IN-2 TFA is a 99mTc-labeled, isonitrile-containing derivative inhibitor of fibroblast activation protein (FAP), used for tumor imaging [1].

SP-13786 is an inhibitor of fibroblast activation protein (FAP) and prolyl oligopeptidase (PREP) with IC50 values ​​of 3.2 nM and 1.8 μM, respectively.