| Drug Name |
Ruxolitinib |
| Drug ID |
BADD_D01978 |
| Description |
Ruxolitinib, formerly known as INCB018424 or INC424, is an anticancer drug and a Janus kinase (JAK) inhibitor. It is a potent and selective inhibitor of JAK1 and JAK2,[A229698] which are tyrosine kinases involved in cytokine signalling and hematopoiesis.[A7450] Myeloproliferative neoplasms, such as myelofibrosis and polycythemia vera, are often characterized by aberrant activation of the JAK-STAT pathway, leading to abnormal blood cell counts and thrombotic complications. By inhibiting JAK1 and JAK2, ruxolitinib works to block the dysregulated cell signalling pathways and prevents abnormal blood cell proliferation.[A229708] Due to a large number of patients with myeloproliferative neoplasms who have JAK2 mutations, ruxolitinib was the first ATP-competitive inhibitor of JAK1 and JAK2 ever developed.[A229938]
Ruxolitinib was first approved for the treatment of adult patients with myelofibrosis by the FDA in 2011, followed by EMA's approval in 2012.[A229708] In 2014, it was approved for the treatment of polycythemia vera in adults who have an inadequate response to or are intolerant of [hydroxyurea] and in 2019, ruxolitinib was approved for use in steroid-refractory acute graft-versus-host disease in adults and children.[L31958] In 2021, ruxolitinib was approved for treatment of mild to moderate atopic dermatitis in patients 12 years and older whose disease was not adequately controlled by topical prescription therapies or when those therapies were not advisable.[L39125] Available as oral tablets, ruxolitinib is commonly marketed under the trade name Jakafi. Ruxolitinib has been investigated to treat patients with coronavirus disease 2019 (COVID-19) accompanied by severe systemic hyperinflammation. In phase II clinical trials, ruxolitinib improved chest computed tomography and improved recovery in patients with lymphopenia.[A229713, A229718] However, phase III clinical trials later determined that ruxolitinib was inadequate in meeting its primary endpoint of reducing the number of hospitalized COVID-19 patients who experienced severe complications.[L31968] Ruxolitinib was not approved as a treatment for COVID-19. The topical formulation of ruxolitinib was investigated to treat vitiligo,[A229723] atopic dermatitis,[A229728] and psoriasis,[A229883] where it showed promising preliminary results in improving the symptoms of inflammatory skin conditions. |
| Indications and Usage |
Ruxolitinib is indicated for the treatment of inte1mediate or high-risk myelofibrosis (MF), including prima1y MF, post-polycythemia vera MF and post-essential thrombocythemia MF in adults.[L31938] It is also indicated to treat disease-related splenomegaly or symptoms in adult patients with these conditions.[L32073]
Ruxolitinib is indicated for the treatment of polycythemia vera (PV) in adults who have had an inadequate response to or are intolerant of hydroxyurea.[L31938]
Ruxolitinib is indicated for the treatment of steroid-refracto1y acute graft-versus-host disease (GVHD) in adult and pediatric patients 12 years and older.[L31938]
Ruxolitinib is indicated for topical non-continuous and short-term treatment of mild to moderate atopic dermatitis in immunocompetent patients who are 12 years and older and whose disease is not adequately controlled with topical prescription therapies or when the topical prescription therapies are not advisable.[L39125] |
| Marketing Status |
approved |
| ATC Code |
D11AH09; L01EJ01 |
| DrugBank ID |
DB08877
|
| KEGG ID |
D09959
|
| MeSH ID |
C540383
|
| PubChem ID |
25126798
|
| TTD Drug ID |
D04LKS
|
| NDC Product Code |
63552-049; 50881-005; 11014-0451; 11014-0452; 50881-015; 11014-0449; 50881-010; 50881-020; 63552-050; 11014-0453; 63552-053; 50881-007; 50881-025; 11014-0450; 63552-051; 63552-052 |
| UNII |
82S8X8XX8H
|
| Synonyms |
ruxolitinib | 3R)-3-cyclopentyl-3-(4-(7H-pyrrolo(2,3-d)pyrimidin-4-yl)pyrazol-1-yl)propanenitrile | ruxolitinib phosphate | ruxolitinib monophosphate | INCB-18424 phosphate | Jakavi | INCB018424 phosphate | INCB-018424 salt | Jakafi | ruxolitinib (as phosphate) | INCB-018424 phosphate | INCB-018424 | INC-424 | INCB-18424 | INC424 | INCB018424 | INCA24 |
