Repositioning Candidate Details
| Candidate ID: | R1451 |
| Source ID: | DB12500 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Fedratinib |
| Synonyms: | Fedratinib |
| Molecular Formula: | C27H36N6O3S |
| SMILES: | CC1=CN=C(NC2=CC=C(OCCN3CCCC3)C=C2)N=C1NC1=CC=CC(=C1)S(=O)(=O)NC(C)(C)C |
| Structure: |
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| DrugBank Description: | Fedratinib, also known as SAR302503 and TG101348, is a tyrosine kinase inhibitor used to treat intermediate-2 and high risk primary and secondary myelofibrosis. It is an anilinopyrimidine derivative. Fedratinib was granted FDA approval on August 16, 2019. |
| CAS Number: | 936091-26-8 |
| Molecular Weight: | 524.678 |
| DrugBank Indication: | Fedratinib is indicated to treat adults with primary or secondary myelofibrosis that is either intermediate-2 or high risk. |
| DrugBank Pharmacology: | Fedratinib is a kinase inhibitor that inhibits cell division and induces apoptosis. Patients taking fedratinib may experience anemia, thrombocytopenia, gastrointestinal toxicity, hepatic toxicity, or elevated amylase and lipase. These effects should be managed by reducing the dose, temporarily stopping the medication, or providing transfusions on a case by case basis. |
| DrugBank MoA: | Fedratinib is an inhibitor of Janus Activated Kinase 2 (JAK2) and FMS-like tyrosine kinase 3. JAK2 is highly active in myeloproliferative neoplasms like myelofibrosis. Fedratinib's inhibition of JAK2 inhibits phosphorylation of signal transducer and activator of transcription (STAT) 3 and 5, which prevents cell division and induces apoptosis. |
| Targets: | Tyrosine-protein kinase JAK2 inhibitor; Receptor-type tyrosine-protein kinase FLT3 inhibitor; Tyrosine-protein kinase JAK1 inhibitor |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S03 | Anti-fibrosis | fibrosis | Angiotensin Receptor Blocker (ARB); CCR2/CCR5 antagonist; Thyroid receptor β agonist; PEGylated human FGF21 analogue; Monoclonal antibody to lysyl oxidase-like 2 (LOXL2); Galectin-3 inhibitor; FGF19 variant | Losartan; Cenicriviroc; VK-2809; MGL-3196; Pegbelfermin; Simtuzumab; GR-MD-02; NGM282 | Details |
| S13 | Anti-apoptosis | hepatocyte apoptosis; hepatic autophagy; apoptosis | Pan-caspase inhibitor | Emricasan | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Diseases ID | DO ID | Disease Name | Definition | Class |
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