FKBP12 Overview
Molecule Name
FK506-binding protein 1A
Synonyms
FKBP1A,FKBP1,Calstabin-1,FKBP12,Rotamase,PKC12,PPIASE
Drug Development Progress
Drugs in Clinical Trials5
Approved Drugs2
Highest Development StageApproved
Target Synonym
Peptidyl-Prolyl Cis-Trans Isomerase FKBP1A，FK506-Binding Protein， T-Cell， 12-KD，FK506-Binding Protein 1A (12kD)，Protein Kinase C Inhibitor 2，FK506-Binding Protein 12，FK506 Binding Protein12，FK506-Binding Protein 1，FKBP12-Exip3，Calstabin 1，PPIASE，PKC12，PKCI2，Tacrolimus Binding Protein 1A，FKBP12C，FK506 Binding Protein 1A， 12kDa，12 KDa FK506-Binding Protein，Immunophilin FKBP12，12 KDa FKBP，Rotamase，FKBP Prolyl Isomerase 1A，FKBP1，FKBP12，FKBP-12，PPIase FKBP1A，FK506-binding protein 1A，Calstabin-1，FKBP-1A，FKBP1A，FK506 Binding Protein 1A
Background
Peptidyl-prolyl cis-trans isomerase FKBP1A, a member of the FKBP-type PPIase family and FKBP1 subfamily, is also known as FK506-binding protein 1A, immunophilin FKBP12 and 12 kDa FK506-binding protein, which contains one PPIase FKBP-type domain. FKBP1A is a cis-trans prolyl isomerase that binds the immunosuppressants FK506 (tacrolimus) and rapamycin (sirolimus).FKBP1A interacts with several intracellular signal transduction proteins including type I TGF-beta receptor. FKBP1A can also interact with multiple intracellular calcium release channels including the tetrameric skeletal muscle ryanodine receptor. Furthermore, FKBP1A can recruite SMAD7 to ACVR1B which prevents the association of SMAD2 and SMAD3 with the activin receptor complex, thereby blocking the activin signal.
FKBP12 Product List
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Clinical Drug Information
| English Name | Research Code | Highest Development Stage | Company | Indication | Clinical Trial |
|---|---|---|---|---|---|
| MAM-1003-1 | MAM-1003-1 | Phase 2 Clinical | Marinomed Biotech AG | Conjunctivitis, Allergic; Rhinitis, Allergic | Details |
| Tacrolimus (novaliq) | NOV-05; NOV05; BTQ2401; BTQ-2401 | Phase 2 Clinical | Novaliq Gmbh | Keratoconjunctivitis; Uveitis; Uveitis, Anterior; Xerophthalmia | Details |
| Plerixafor/Tacrolimus Hydrate | MRG-001(MedRegen); AMD3100+FK506 | Phase 2 Clinical | MedRegen LLC | Abdominal Injuries; Amyotrophic Lateral Sclerosis; Coronavirus Disease 2019 (COVID-19); Cytokine Release Syndrome; Hepatitis, Alcoholic; Motor Neuron Disease; Respiratory Distress Syndrome, Adult; Respiratory Insufficiency; Respiratory Tract Diseases; Wounds and Injuries | Details |
| Rimiducid | AP-1903 | Phase 2 Clinical | Ariad Pharmaceuticals Inc, Bellicum Pharmaceuticals Inc | Anemia, Aplastic; Anemia, Diamond-Blackfan; Anemia, Sickle Cell; Blastic Plasmacytoid Dendritic Cell Neoplasm; Bone Marrow Neoplasms; Colorectal Neoplasms; Congenital Bone Marrow Failure Syndromes; Cytopenia; Fanconi Anemia; Graft vs Host Disease; Hematologic Neoplasms; Hemoglobinopathies; Hodgkin Disease; Immune System Diseases; Immunoproliferative Disorders; Leukemia; Leukemia, Biphenotypic, Acute; Leukemia, Lymphoid; Leukemia, Myelogenous, Chronic; Leukemia, Myeloid, Acute; Leukemia, Myelomonocytic, Chronic; Lymphohistiocytosis, Hemophagocytic; Lymphoma; Lymphoma, B-Cell; Lymphoma, Non-Hodgkin; Melanoma; Metabolic Diseases; Multiple Myeloma; Myelodysplastic Syndromes; Myelodysplastic-Myeloproliferative Diseases; Myeloproliferative Disorders; Neoplasm, Residual; Neuroblastoma; Osteopetrosis; Osteosarcoma; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Primary Immunodeficiency Diseases; Prostatic Neoplasms; Prostatic Neoplasms, Castration-Resistant; Sarcoma; Solid tumours; Thalassemia; Uveal melanoma | Details |
| SQ-708 | SQ-708 | Phase 1 Clinical | Shenyang Xingqi Pharmaceutical Co Ltd | Keratoplasty rejection | Details |
Marketed Drug Information
| English Name | Research Code | Highest Development Stage | Company | First Brand Name | First Approved Country | First Indication | First Approved Company | First Approved Date | Indication | Clinical Trial |
|---|---|---|---|---|---|---|---|---|---|---|
| Tacrolimus Hydrate | FK-506; MR-4; RTU-007; LCP-Tacro; FR-900506; L-679934; FK-506MR; FK-506E | Approved | Astellas Pharma Inc | Protopy, Graceptor (as hydrate), TacroBell, Advagraf, Envarsus, Modigraf, Astagraf XL, Protopic, Prograf (as hydrate), Hecoria (as hydrate), Hexal, Envarsus XR, Talymus, 普乐可复 | United States | Rejection of liver transplantation; Rejection in heart transplantation; Rejection of renal transplantation | Astellas Pharma Us Inc | 1994-04-08 | Amputation, Traumatic; Arthritis, Rheumatoid; Asthma; Bone marrow transplant rejection; Brain Death; Burns; Colitis, Ulcerative; Conjunctivitis; Crohn Disease; Dermatitis, Atopic; Dermatomyositis; Dry Eye Syndromes; Edema; Encephalitis; Genital Diseases, Male; Glomerulonephritis, IGA; Graft vs Host Disease; Hamman-Rich Syndrome; Infertility, Female; Keratoconjunctivitis; Keratoconjunctivitis Sicca; Keratoplasty rejection; Kidney Diseases; Leukemia, Myelogenous, Chronic; Leukemia, Myeloid, Acute; Leukemia, Myelomonocytic, Chronic; Liver Failure; Lung Diseases, Interstitial; Lupus Erythematosus, Cutaneous; Lupus Nephritis; Medication Adherence; Myasthenia Gravis; Myelodysplastic Syndromes; Nephrotic Syndrome; Ocular inflammation; Peripheral Nerve Injuries; Polymyositis; Primary Graft Dysfunction; Primary Myelofibrosis; Psoriasis; Pulmonary Arterial Hypertension; Rejection in heart transplantation; Rejection of renal transplantation; Rejection of liver transplantation; Rejection of lung transplantation; Rejecti | Details |
| Pimecrolimus | SDZ-ASM-981; ASM-998; ASM-981 | Approved | Novartis Pharma Ag | Elidel | United States | Dermatitis, Atopic | Bausch & Lomb (Singapore) Pvi Ltd | 2001-12-13 | Dermatitis; Dermatitis, Atopic; Dermatitis, Perioral; Dermatitis, Seborrheic; Eczema; Exanthema; Keratoconjunctivitis Sicca; Lichen Planus, Oral; Netherton Syndrome; Pityriasis; Prurigo Nodularis; Vitiligo | Details |