FAP Overview
Molecule Name
Prolyl endopeptidase FAP
Synonyms
FAP,FAPalpha,SIMP,Seprase,APCE
Drug Development Progress
Drugs in Clinical Trials87
Approved Drugs0
Highest Development StagePhase 3 Clinical
Target Synonym
Post-Proline Cleaving Enzyme，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，170 kDa melanoma membrane-bound gelatinase，Seprase，Gelatine degradation protease FAP，Dipeptidyl peptidase FAP，Fibroblast activation protein alpha，APCE，Integral membrane serine protease，Surface-expressed protease，FAP
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.
FAP Product List
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Clinical Drug Information
| English Name | Research Code | Highest Development Stage | Company | Indication | Clinical Trial |
|---|---|---|---|---|---|
| 18F-LNC1007 | 18F-LNC1007; 18F-FAPI-RGD | Phase 3 Clinical | Yantai Lannacheng Biotechnology Co Ltd | Carcinoma, Renal Cell; Diagnostic agents; Neoplasms; Solid tumours | Details |
| [18F]FAPI-74 | Fluor-18-FAPI-74; F-18]FAPI-74; FAPI-74; [18F]FAPI-74 | Phase 3 Clinical | University Of Heidelberg | Adenocarcinoma; Biliary Tract Neoplasms; Breast Neoplasms; Carcinoma, Hepatocellular; Carcinoma, Lobular; Carcinoma, Pancreatic Ductal; Cholangiocarcinoma; Colorectal Neoplasms; Dermatomyositis; Esophageal Neoplasms; Gastrointestinal Neoplasms; Mesothelioma; Ovarian Neoplasms; Pancreatic Neoplasms; Sarcoma; Stomach Neoplasms; Urinary Bladder Neoplasms | Details |
| [18F]fibronstatin | 18F-LNC1005; LNC-1005 | Phase 3 Clinical | Yantai Lannacheng Biotechnology Co Ltd | Diagnostic agents; Solid tumours; Stomach Neoplasms | Details |
| Talabostat | VbP; PT-100; BXCL-701 | Phase 2 Clinical | Point Therapeutics | Adenocarcinoma; Carcinoma, Non-Small-Cell Lung; Carcinoma, Pancreatic Ductal; Carcinoma, Small Cell; CNS Embryonal Tumor; Kidney Neoplasms; Leukemia, Lymphocytic, Chronic, B-Cell; Leukemia, Myeloid, Acute; Liver Neoplasms; Lung Neoplasms; Melanoma; Myelodysplastic Syndromes; Neoplasm Metastasis; Neoplasms, Germ Cell and Embryonal; Neuroblastoma; Neuroendocrine Tumors; Ovarian Neoplasms; Pancreatic Neoplasms; Prostatic Neoplasms; Sarcoma; Skin Neoplasms; Solid tumours | Details |
| MP-0317 | MP-0317 | Phase 2 Clinical | Molecular Partners Ag | Biliary Tract Neoplasms; Solid tumours | Details |
| GPN0-1530 | GPN01530; GPN0-1530 | Phase 2 Clinical | Grand Pharmaceutical （China） Co Ltd | Solid tumours | Details |
| 68Ga-FAP-RGD | 68Ga-FAP-RGD | Phase 2 Clinical | First Affiliated Hospital Of Fujian Medical University | Neoplasms | Details |
| 177Lu-D7ND | 177Lu-D7ND | Phase 2 Clinical | The First Affiliated Hospital of Xi'an Jiaotong University | Solid tumours | Details |
| [212Pb]Pb-PSV359 | [212Pb]Pb-PSV359 | Phase 2 Clinical | Perspective Therapeutics Inc | Carcinoma, Pancreatic Ductal; Colorectal Neoplasms; Esophageal Neoplasms; Head and Neck Neoplasms; Mesothelioma; Ovarian Neoplasms; Sarcoma; Stomach Neoplasms | Details |
| [203Pb]Pb-PSV359 | [203Pb]Pb-PSV359; [203Pb]-PSV359 | Phase 2 Clinical | Perspective Therapeutics Inc | Carcinoma, Pancreatic Ductal; Colorectal Neoplasms; Esophageal Neoplasms; Head and Neck Neoplasms; Mesothelioma; Ovarian Neoplasms; Sarcoma; Stomach Neoplasms | Details |
| 68Ga-NI-FAPI | 68Ga-NI-FAPI | Phase 2 Clinical | First Affiliated Hospital Of Fujian Medical University | Cardiomyopathy, Hypertrophic; Cardiovascular Diseases; Hypoxia; Immune System Diseases; Neoplasms; Pulmonary Fibrosis; Rheumatic Diseases | Details |
| HRS-6768 | HRS-6768; HRS6768 | Phase 2 Clinical | Tianjin Hengrui Pharmaceutical Co Ltd | Solid tumours | Details |
| 68Ga-TCR-FAPI | 68Ga-TCR-FAPI | Phase 2 Clinical | Tumor Research Institute Chinese Academy Of Medical Sciences | Medullary thyroid cancer (MTC); Neoplasms | Details |
| NTI-1309 | LNTH-1363S; NTI-1309; 64Cu-LNTH-1363S | Phase 2 Clinical | Noria Therapeutics Inc | Colorectal Neoplasms; Esophageal Neoplasms; Pancreatic Neoplasms; Sarcoma; Stomach Neoplasms | Details |
| AZD-2389 | AZD2389; AZD-2389 | Phase 2 Clinical | Astrazeneca Plc | Hepatic Insufficiency; Liver Cirrhosis; Liver Diseases | Details |
| AAA-614 | AAA-614; FAP-2286; Lu-FAP-2286 | Phase 2 Clinical | Novartis Ag | Carcinoma, Non-Small-Cell Lung; Carcinoma, Pancreatic Ductal; Solid tumours | Details |
| 68Ga-FAPI(Peking Union Medical College Hospital) | 68Ga-FAPI(Peking Union Medical College Hospital) | Phase 2 Clinical | Peking Union Medical College Hospital | Neoplasm Metastasis; Sjogren's Syndrome | Details |
| 177Lu-EB-FAPI | 177Lu-EB-FAPI | Phase 2 Clinical | Zhejiang University | Carcinoma, Pancreatic Ductal; Cholangiocarcinoma; Pancreatic Neoplasms | Details |
| 177Lu-DOTA-EB-FAPI | Phase 2 Clinical | The First Affiliated Hospital Of Xiamen University | Adenocarcinoma, Follicular; Oncocytic cell carcinoma of the thyroid; Solid tumours; Thyroid Cancer, Papillary; Thyroid Neoplasms | Details | |
| SHR-7367 | SHR7367; SHR-7367 | Phase 2 Clinical | Shanghai Hengrui Pharmaceutical Co Ltd | Neoplasms; Solid tumours | Details |
| 68Ga-FAP-2286 | 68Ga-FAP-2286; 68-Ga-FAP-2286 | Phase 2 Clinical | 3B Pharmaceuticals GmbH | Neoplasm Metastasis; Solid tumours | Details |
| 68Ga-FAPI-46 | [68Ga]FAPI-46; 68Ga-FAPI-46 | Phase 2 Clinical | Karolinska University Hospital | Adenomatous Polyposis Coli; Alveolitis, Extrinsic Allergic; Bile Duct Neoplasms; Carcinoma, Hepatocellular; Carcinoma, Intraductal, Noninfiltrating; Carcinoma, Ovarian Epithelial; Carcinoma, Pancreatic Ductal; Crohn Disease; Esophageal Neoplasms; Idiopathic Interstitial Pneumonias; Inflammatory Bowel Diseases; Intestinal Fibrosis; Lung Diseases, Interstitial; Melanoma; Metabolic Dysfunction-Associated Steatotic Liver Disease; Neoplasms; Ovarian Neoplasms; Pancreatic Neoplasms; Pneumoconiosis; Pulmonary Fibrosis; Radiation Pneumonitis; Solid tumours; Stomach Neoplasms | Details |
| 177Lu-FAP-2286 | 177Lu-FAP-2286 | Phase 2 Clinical | 3B Pharmaceuticals GmbH | Neoplasms; Solid tumours | Details |
| NG-641 | EnAd-FAP-BiTE; EnAd-FAP-Tac; NG-641; NG-aFAP | Phase 1 Clinical | Akamis Bio Ltd | Neoplasm Metastasis; Neoplasms, Glandular and Epithelial; Squamous Cell Carcinoma of Head and Neck | Details |
| Simlukafusp alfa | FAP-IL2v; RG-7461; aFAP-IL2v; RO-6874281; FAP-IL2v FP | Phase 1 Clinical | F. Hoffmann-La Roche Ltd | Breast Neoplasms; Carcinoma, Renal Cell; Esophageal Neoplasms; Head and Neck Neoplasms; Melanoma; Solid tumours; Uterine Cervical Neoplasms | Details |
| 177Lu-DOTAGA.FAPi | TLX400; TLX-400; 177Lu-TLX400 | Phase 1 Clinical | Johannes Gutenberg University Of Mainz | Medullary thyroid cancer (MTC); Metastatic breast cancer; Urinary Bladder Neoplasms | Details |
| CD137/FAP bispecific agonist antibody (Boehringer Ingelheim International) | Phase 1 Clinical | Boehringer Ingelheim International Gmbh | Neoplasms | Details | |
| PSMA/NKG2DL/FAP-targeted Hi-TCR-T cells | Phase 1 Clinical | Shenzhen Misheng Biotechnology Co Ltd | Prostatic Neoplasms; Solid tumours | Details | |
| 68Ga-PNT-6555 | Phase 1 Clinical | Point Biopharma Inc | Carcinoma, Pancreatic Ductal; Colorectal Neoplasms; Esophageal Neoplasms; Melanoma; Sarcoma; Solid tumours | Details | |
| 68Ga-FAPI-XT-117 | Phase 1 Clinical | Beijing Xiantong International Technology Co Ltd | Solid tumours | Details | |
| OMTX-705 | OMTX-705 | Phase 1 Clinical | Oncomatryx Biopharma Sl | Adenocarcinoma; Solid tumours | Details |
| CAR-DC Targeting FAP therapy (Second Affiliated Hospital School Of Zhejiang University School Of Medicine) | Phase 1 Clinical | Second Affiliated Hospital School Of Zhejiang University School Of Medicine | Idiopathic Pulmonary Fibrosis; Shock, Cardiogenic; ST Elevation Myocardial Infarction | Details | |
| CD40xFAP bispecific antibody (Bristol-Myers Squibb Company) | Phase 1 Clinical | Bristol-Myers Squibb Company | Solid tumours | Details | |
| 177Lu-JH040182 | 177Lu-JH040182; 177LuJH040182; [177Lu]-JH04 | Phase 1 Clinical | Bivision Biomedical Technology (Shanghai) Co Ltd | Solid tumours | Details |
| 177Lu-BRP-010030 | 177LuBRP010030; 177Lu-BRP-010030 | Phase 1 Clinical | BoomRay Pharmaceuticals Co Ltd | Solid tumours | Details |
| LY-4337713 | LY4337713; LY-4337713 | Phase 1 Clinical | Eli Lilly And Company | Breast Neoplasms; Cholangiocarcinoma; Colorectal Neoplasms; Esophageal Neoplasms; Ovarian Neoplasms; Pancreatic Intraductal Neoplasms; Stomach Neoplasms | Details |
| MP-0310 | MP-0310; AMG-506 | Phase 1 Clinical | Amgen Inc, Molecular Partners Ag | Solid tumours | Details |
| 68Ga-FAPI-GP | Phase 1 Clinical | Affiliated Hospital of Guilin Medical University | Solid tumours | Details | |
| 177Lu-FAPI-FUSCC | Phase 1 Clinical | Fudan University Shanghai Cancer Center | Solid tumours | Details | |
| 225Ac-FAPI-XT | XT117 | Phase 1 Clinical | Cancer Hospital of Shandong First Medical University | Solid tumours | Details |
| 68Ga-DOTA-FAPI-04 | 68Ga-DOTA-FAPI-04 | Phase 1 Clinical | The First Affiliated Hospital Of Xiamen University | Neuroendocrine Tumors | Details |
| 68Ga-GP-01 | 68Ga-GP-01 | Phase 1 Clinical | Chengdu Shetai Medical Technology Co Ltd | Solid tumours | Details |
| 177Lu-NRT6020 | 177Lu-NRT6020 | Phase 1 Clinical | Chengdu New Radiomedicinetechnology Co Ltd | Solid tumours | Details |
| 68Ga-NRT6020 | 68Ga-NRT6020 | Phase 1 Clinical | Chengdu New Radiomedicinetechnology Co Ltd | Solid tumours | Details |
| 3BP-4961 | 3BP-4961; SPECTROFAP; 99mTc-3BP-4961 | Phase 1 Clinical | 3B Pharmaceuticals GmbH | Neoplasms | Details |
| AVA-6103 | AVA6103; AVA-6103 | Phase 1 Clinical | Avacta Group PLC | Adenocarcinoma; Carcinoma, Pancreatic Ductal; Esophageal Neoplasms; Neoplasms; Pancreatic Neoplasms; Small Cell Lung Carcinoma; Solid tumours; Stomach Neoplasms; Uterine Cervical Neoplasms | Details |
| [177Lu]Lu-OncoFAP-23 | [177Lu]Lu-OncoFAP-23 | Phase 1 Clinical | Philogen Spa | Adenomatous Polyposis Coli | Details |
| 177Lu-FAPI-RGD | 177Lu-FAPI-RGD; [177Lu]-FAPI-RGD | Phase 1 Clinical | Peking Union Medical College Hospital | Neoplasms | Details |
| 177Lu-JH04 | 177Lu-JH04 | Phase 1 Clinical | First Affiliated Hospital Of Fujian Medical University | Neoplasms | Details |
| [68Ga]Ga-NNS309 | [68Ga]Ga-NNS309 | Phase 1 Clinical | Novartis Pharma Ag | Breast Neoplasms; Carcinoma, Non-Small-Cell Lung; Carcinoma, Pancreatic Ductal; Colorectal Neoplasms; Triple Negative Breast Neoplasms | Details |
| [177Lu]Lu-NNS309 | [177Lu]Lu-NNS309; FXX489; FXX-489 | Phase 1 Clinical | Novartis Pharma Ag | Breast Neoplasms; Carcinoma, Non-Small-Cell Lung; Carcinoma, Pancreatic Ductal; Colorectal Neoplasms; Large intestine neoplasm; Triple Negative Breast Neoplasms | Details |
| Lutetium [177Lu]-FAP-75 | Lutetium [177Lu]-FAP-75 | Phase 1 Clinical | Fudan University | Solid tumours | Details |
| 68Ga-JH04 | 68Ga-JH04; JH-04 | Phase 1 Clinical | Bivision Pharmaceuticals Inc | Neoplasms | Details |
| 68Ga-DOTA-NI-FAPI04 | 68Ga-DOTA-NI-FAPI04 | Phase 1 Clinical | First Affiliated Hospital Of Fujian Medical University | Neoplasms | Details |
| 68Ga-FAPI-JH04 | 68Ga-FAPI-JH04 | Phase 1 Clinical | First Affiliated Hospital Of Fujian Medical University | Neoplasms | Details |
| 68Ga-PSFA | 68Ga-PSFA | Phase 1 Clinical | First Affiliated Hospital Of Chongqing Medical University | Adenomatous Polyposis Coli | Details |
| 68 Ga-OncoFAP-DOTAGA | 68 Ga-OncoFAP | Phase 1 Clinical | Blue Earth Diagnostics, Philochem | Solid tumours | Details |
| 18F-AlF-FAPi-04 | 18F-AlF-FAPi-04 | Phase 1 Clinical | Affiliated Hospital Of North Sichuan Medical College | Solid tumours | Details |
| 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 |
| [64Cu]Cu-XT117 | [64Cu]Cu-XT117; 64Cu-FAPI-XT117 | Phase 1 Clinical | Beijing Xiantong International Technology Co Ltd | Solid tumours | Details |
| [177Lu]Lu-XT117 | XTR-017; XTR017; [177Lu]Lu-XT117 | Phase 1 Clinical | Beijing Xiantong International Technology Co Ltd | Solid tumours | Details |
| RTX-1363-S | RTX-1363S; RTX-1363-S | Phase 1 Clinical | Ratio Therapeutics Inc | Breast Neoplasms; Lung Neoplasms; Pancreatic Neoplasms; Stomach Neoplasms | Details |
| 68Ga/64Cu-FAPI-XT117 | 68Ga/64Cu-FAPI-XT117 | Phase 1 Clinical | Beijing Xiantong International Technology Co Ltd | Solid tumours | Details |
| 177Lu-LNC1004 | 177Lu-LNC1004; 177Lu-LNC-1004 | Phase 1 Clinical | Yantai Lannacheng Biotechnology Co Ltd | Solid tumours | Details |
| 68Ga-LNC-1007 | 68Ga-FAPI-RGD; 68Ga-LNC-1007 | Phase 1 Clinical | Yantai Lannacheng Biotechnology Co Ltd | Carcinoma, Renal Cell; Neoplasms | Details |
| BI-765179 | BI-765179 | Phase 1 Clinical | Boehringer Ingelheim International Gmbh | Neoplasms; Squamous Cell Carcinoma of Head and Neck | Details |
| RO-7300490 | RO-7300490; RG-6189; FAP-CD40; FAP-huCD40 | Phase 1 Clinical | F. Hoffmann-La Roche Ltd | Solid tumours | Details |
| 177Lu-DOTA-FAPI | 177Lu-DOTA-2P | Phase 1 Clinical | The First Affiliated Hospital Of Xiamen University | Neoplasm Metastasis; Solid tumours | Details |
| RO-7122290 | RO-7122290; RG-7827 | Phase 1 Clinical | F. Hoffmann-La Roche Ltd | Colorectal Neoplasms | Details |
| anti-BCMA/NKG2DL/FAP TCR T-cell therapy (Guangdong VitaLife) | Clinical | Guangdong Vitalife Biotechnology Co Ltd | Multiple Myeloma | Details | |
| 68Ga-FAPI(Meander Medical Center) | 68Ga-FAPI | Clinical | Meander Medical Center | Carcinoma, Non-Small-Cell Lung | Details |
| 68Ga-BR-54 | 68Ga-BR-54 | Clinical | BoomRay Pharmaceuticals Co Ltd | Neoplasms | Details |
| 68Ga-DOTA-GPFAPI-04 | [68Ga]Ga-DOTA-GPFAPI-04; 68Ga-GPFAPI-04 | Clinical | Guangdong Provincial People'S Hospital, Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Neoplasm Metastasis; Neoplasms | Details |
| 90Y-FAPI-04 | Clinical | Heidelberg University Hospital | Breast Neoplasms | Details | |
| 68Ga-NOTA-FAPI04 | Clinical | Beijing Cancer Hospital | Lymphoma | Details | |
| 68Ga-DOTA-FAPI-46 | Clinical | The First Affiliated Hospital Of Xiamen University | Neoplasms | Details | |
| 68Ga-DOTA-2P(FAPI)2 | Clinical | The First Affiliated Hospital Of Xiamen University | Neoplasms | Details | |
| [18F]AlF-NOTA-FAPI-04 | Clinical | Sichuan Provincial People'S Hospital | Kidney Diseases | Details | |
| 99mTc-HFAPI | Clinical | Peking Union Medical College Hospital | Pulmonary Fibrosis | Details | |
| 68Ga/18F-FAPI-04 | Clinical | Nanjing First Hospital, Nanjing Medical University | Endomyocardial Fibrosis | Details | |
| 68Ga-FAPI-LM3 | 68Ga-FAPI-LM3 | Clinical | The First Affiliated Hospital Of Xiamen University | Adenomatous Polyposis Coli | Details |
| [18F]AlF-FAPI-74 | 18F-AlF-FAPI-74; [18F]-ALF-FAPI-74 | Clinical | Umc Utrecht | Colorectal Neoplasms | Details |
| XTR-016 | XTR-016; XTR016 | Clinical | Beijing Xiantong International Technology Co Ltd | Solid tumours | Details |
| 177Lu-BRP-010 | BRP-010; 177Lu-BRP-010 | Clinical | BoomRay Pharmaceuticals Co Ltd | Solid tumours | Details |
| 68Ga-BRP-010 | BRP-010; 68Ga-BRP-010 | Clinical | BoomRay Pharmaceuticals Co Ltd | Solid tumours | Details |
| [90Y] YFAPI-46 | Clinical | German Cancer Consortium (Dktk), University of Duisburg-Essen | Solid tumours | Details | |
| 3BP-3940 | 3BP-3940 | Clinical | 3B Pharmaceuticals GmbH, Johannes Gutenberg University Of Mainz | Neoplasms | Details |