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FAP

Brief Information

Name:Fibroblast activation protein alpha
Target Synonym:EC:3.4.21.-,EC:3.4.21.26,EC:,3.4.21.-,EC:3.4.14.5,170 kDa melanoma membrane-bound gelatinase,Seprase,Dipeptidyl peptidase FAP,APCE,Integral membrane serine protease,FAP,Post-Proline Cleaving Enzyme,Gelatine degradation protease FAP,Fibroblast activation protein alpha,Surface-expressed protease,FAPalpha,SIMP,Fibroblast Activation Protein, Alpha,Serine Integral Membrane Protease,Prolyl Endopeptidase FAP,EC 3.4.21.26,EC 3.4.14.5,EC 3.4.21.-,DPPIV,FAPA,EC:,3.4.14.5
Number of Launched Drugs:0
Number of Drugs in Clinical Trials:27
Lastest Research Phase:Phase 2 Clinical

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Part of Bioactivity data

FAP-HP245-Cell-based assay
FACS assay shows that recombinant Biotinylated FACS

5e5 of anti-FAP CAR-293 cells were stained with 100 μL of 1:25 dilution (4 μL stock solution in 100 μL FACS buffer) of PE-Labeled Human FAP, His Tag (Cat. No. FAP-HP245) and negative control protein respectively. PE signal was used to evaluate the binding activity (QC tested).

FAP-HF263-Cell-based assay
 FAP FACS

2e5 of anti-FAP CAR-293 cells were stained with 100 μL of 3 μg/mL of FITC-Labeled Human FAP, Fc Tag (Cat. No. FAP-HF263) and negative control protein respectively, FITC signal was used to evaluate the binding activity (QC tested).

FAP-R5246-SPR
 FAP SPR

Anti-FAP Antibody, Mouse IgG2a (FAP5) captured on CM5 chip via anti-mouse antibodies surface can bind Rat FAP, His Tag (Cat. No. FAP-R5246) with an affinity constant of 0.839 nM as determined in a SPR assay (Biacore 8K) (Routinely tested).

FAP-C52H3-SPR
 FAP SPR

Anti-FAP Antibody, Mouse IgG2a (FAP5) captured on CM5 chip via anti-mouse antibodies surface can bind Cynomolgus FAP, His Tag (Cat. No. FAP-C52H3) with an affinity constant of 3.10 nM as determined in a SPR assay (Biacore 8K) (Routinely tested).

Synonym Name

FAP,FAPalpha,SIMP,Seprase,APCE

Background

FAP (also known as seprase) is a Type II transmembrane serine protease. Both plasma membrane and soluble forms exhibit post-proline cleaving endopeptidase activity, with a marked preference for Ala/Ser-Gly-Pro-Ser/Asn/Ala consensus sequences. Degrade also gelatin, heat-denatured type I collagen. Also has dipeptidyl peptidase activity, with a preference for Ala-Pro, Ile-Pro, Gly-Pro, Arg-Pro and Pro-Pro. The plasma membrane form, in association with either DPP4, PLAUR or integrins, is involved in the pericellular proteolysis of the extracellular matrix (ECM), and hence promotes cell adhesion, migration and invasion through the ECM. Promotes glioma cell invasion through the brain parenchyma by degrading the proteoglycan brevican. Acts as a tumor suppressor in melanocytic cells through regulation of cell proliferation and survival in a serine protease activity-independent manner.

Clinical and Translational Updates

Clinical Drug Information

Name Research Code Research Phase Company Indications Clinical Trials
177Lu-EB-FAPI(Peking Union Medical College Hospital) 177Lu-EB-FAPI(Peking Union Medical College Hospital) Phase 1 Clinical Peking Union Medical College Hospital Neoplasm Metastasis Details
Simlukafusp alfa FAP-IL2v; RG-7461; aFAP-IL2v; RO-6874281; FAP-IL2v FP Phase 1 Clinical F. Hoffmann-La Roche Ltd Head and Neck Neoplasms; Solid tumours; Carcinoma, Renal Cell; Esophageal Neoplasms; Breast Neoplasms; Uterine Cervical Neoplasms; Melanoma Details
177Lu-PNT6555(Point Biopharma) PNT-6555 Phase 1 Clinical Point Biopharma Inc Solid tumours; Squamous Cell Carcinoma of Head and Neck; Esophageal Neoplasms; Sarcoma; Cholangiocarcinoma; Colorectal Neoplasms; Carcinoma, Pancreatic Ductal; Melanoma Details
RO-7122290 RO-7122290; RG-7827 Phase 2 Clinical F. Hoffmann-La Roche Ltd Colorectal Neoplasms Details
68Ga-FAPI(Peking Union Medical College Hospital) 68Ga-FAPI(Peking Union Medical College Hospital) Phase 1 Clinical Peking Union Medical College Hospital Neoplasm Metastasis Details
Talabostat PT-100; BXCL-701 Phase 2 Clinical Midatech Pharma Plc, Bioxcel Therapeutics Inc Brain Neoplasms; Carcinoma, Non-Small-Cell Lung; Neoplasm Metastasis; Melanoma; Adenocarcinoma; Leukemia, Lymphocytic, Chronic, B-Cell; Neoplasms, Germ Cell and Embryonal; Carcinoma, Small Cell; Lung Neoplasms; Carcinoma, Pancreatic Ductal; Leukemia, Myeloid, Acute; Prostatic Neoplasms; Solid tumours; Neuroblastoma; Sarcoma; Neuroendocrine Tumors; Central Nervous System Neoplasms; Pancreatic Neoplasms; Skin Neoplasms; Myelodysplastic Syndromes; Kidney Neoplasms; Liver Neoplasms; Ovarian Neoplasms Details
68Ga/64Cu-FAPI-XT117 68Ga/64Cu-FAPI-XT117 Phase 1 Clinical Pla General Hospital, Sinotau Pharmaceutical Group Solid tumours Details
18F-AlF-FAPi-04 18F-AlF-FAPi-04 Phase 1 Clinical Affiliated Hospital Of North Sichuan Medical College Solid tumours Details
68Ga-FAPI-RGD 68Ga-FAPI-RGD Phase 1 Clinical Peking Union Medical College Hospital Lung Neoplasms Details
AAA-614 AAA-614 Phase 1 Clinical Novartis Ag Solid tumours Details
NG-641 EnAd-FAP-BiTE; EnAd-FAP-Tac; NG-641; NG-aFAP Phase 1 Clinical Akamis Bio Ltd, University Of Oxford Squamous Cell Carcinoma of Head and Neck; Neoplasms, Glandular and Epithelial; Neoplasm Metastasis Details
177Lu-FAP-2286 177Lu-FAP-2286 Phase 2 Clinical 3B Pharmaceuticals GmbH Solid tumours Details
MP-0317 MP-0317 Phase 1 Clinical Molecular Partners Ag Solid tumours; Neoplasms Details
MP-0310 MP-0310; AMG-506 Phase 1 Clinical Molecular Partners Ag, Amgen Inc Solid tumours Details
3BP-3940 3BP-3940 Clinical Johannes Gutenberg University Of Mainz, 3B Pharmaceuticals GmbH Neoplasms Details
Nectin4/FAP-targeted CAR-T cell therapy (The Sixth Affiliated Hospital of Wenzhou Medical University) Phase 1 Clinical Wenzhou Medical University, The Sixth Affiliated Hospital Of Wenzhou Medical University Solid tumours Details
OMTX-705 OMTX-705 Phase 1 Clinical Oncomatryx Biopharma Sl Solid tumours Details
68Ga-FAPI-46 Phase 2 Clinical Karolinska University Hospital Pancreatic Neoplasms; Pneumoconiosis; Alveolitis, Extrinsic Allergic; Carcinoma, Pancreatic Ductal; Bile Duct Neoplasms; Pulmonary Fibrosis; Lung Diseases, Interstitial; Carcinoma, Ovarian Epithelial; Neoplasms; Adenomatous Polyposis Coli; Pneumonia; Stomach Neoplasms; Esophageal Neoplasms; Radiation Pneumonitis; Non-alcoholic Fatty Liver Disease; Idiopathic Interstitial Pneumonias; Ovarian Neoplasms Details
177Lu-EB-FAPI 177Lu-EB-FAPI Phase 1 Clinical Zhejiang University Pancreatic Neoplasms; Cholangiocarcinoma Details
177Lu-DOTA-EB-FAPI Phase 1 Clinical Solid tumours; Adenocarcinoma, Follicular; Thyroid Neoplasms; Thyroid Cancer, Papillary Details
[18F]FAPI-74 FAPI-74; [18F]FAPI-74 Phase 2 Clinical Sofie Biliary Tract Neoplasms; Stomach Neoplasms; Pancreatic Neoplasms; Cholangiocarcinoma; Colorectal Neoplasms; Carcinoma, Pancreatic Ductal; Carcinoma, Hepatocellular; Gastrointestinal Neoplasms Details
68 Ga-OncoFAP-DOTAGA 68 Ga-OncoFAP Phase 1 Clinical Blue Earth Diagnostics, Philochem Solid tumours Details
177Lu-LNC1004 177Lu-LNC1004; 177Lu-LNC-1004 Phase 1 Clinical Shanghai Lannacheng Biotechnology Co Ltd Solid tumours Details
RTX-1363-S RTX-1363S; RTX-1363-S Phase 1 Clinical Ratio Therapeutics Inc Stomach Neoplasms; Pancreatic Neoplasms; Breast Neoplasms; Lung Neoplasms Details
RO-7300490 RO-7300490; RG-6189 Phase 1 Clinical F. Hoffmann-La Roche Ltd Solid tumours; Neoplasms Details
68Ga-FAP-2286 68Ga-FAP-2286; 68-Ga-FAP-2286 Phase 2 Clinical 3B Pharmaceuticals GmbH Solid tumours; Neoplasm Metastasis Details
[90Y] YFAPI-46 Clinical German Cancer Consortium (Dktk), University of Duisburg-Essen Solid tumours Details

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