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Jakafi

Jakafi structure

CAS No:
1092939-17-7
Formula:
C17H18N6.H3O4P
Chemical Name:
Jakafi
Synonyms:
1H-Pyrazole-1-propanenitrile,β-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-,(βR)-,phosphate (1:1);Jakafi;Ruxolitinib phosphate;INCB 018424 phosphate;INC 424 phosphate;Jakavi
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

ChEBI: A phosphate salt obtained by reaction ruxolitinib with one equivalent of phosphoric acid. Used for the treatment of patients with intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essent al thrombocythemia myelofibrosis.Ruxolitinib, (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3- cyclopentylpropanenitrile phosphate, has a molecular weight of 404.36 kDa. Ruxolitinib is soluble in aqueous solutions at pH

Ruxolitinib phosphate is a phosphate salt obtained by reaction ruxolitinib with one equivalent of phosphoric acid. Used for the treatment of patients with intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essential thrombocythemia myelofibrosis. It has a role as an antineoplastic agent and an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor. It contains a ruxolitinib.|Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Ruxolitinib specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies.

Jakafi Basic Attributes

Molecular Weight：

404.360201

Exact Mass：

404.136200

UNII：

436LRU32H5

NCI Thesaurus Code：

C97937

ATC Code：

L01EJ01

HScode：

29331990

Characteristics

PSA：

161

XLogP3：

2.53778

Safety Information

Precautionary statement(s)：

P201, P202, P260, P264, P270, P281, P301+P310, P301+P312, P308+P313, P314, P321, P330, P405, P501

Hazard Statements：

H301

GHS Classification：

|Danger|H301 (66.67%): Toxic if swallowed [Danger Acute toxicity, oral]|P201, P202, P260, P264, P270, P281, P301+P310, P301+P312, P308+P313, P314, P321, P330, P405, and P501|Aggregated GHS information provided by 3 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Myelofibrosis (MF)Jakavi is indicated for the treatment of disease related splenomegaly or symptoms in adult patients with primary myelofibrosis (also known as chronic idiopathic myelofibrosis), post polycythaemia vera myelofibrosis or post essential thrombocythaemia myelofibrosis.Polycythaemia vera (PV)Jakavi is indicated for the treatment of adult patients with polycythaemia vera who are resistant to or intolerant of hydroxyurea. |Treatment of chronic Graft versus Host Disease (cGvHD)|Treatment of acute graft-versus-host disease (aGvHD)|Drug: Ruxolitinibphosphate

Jakafi Use and Manufacturing

Uses

The phosphate salt of Ruxolitinib (R702000). Ruxolitinib is a selective Janus tyrosine kinase (JAK1 and JAK2) inhibitor used in the treatment of myeloproliferative neoplasms and psoriasis.

Use Classification：

Human drugs -> Jakavi -> EMA Drug Category|Antineoplastic agents -> Human pharmacotherapeutic group|Human drugs -> Rare disease (orphan)|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:404.4
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:8
Rotatable Bond Count:4
Exact Mass:404.13619017
Monoisotopic Mass:404.13619017
Topological Polar Surface Area:161
Heavy Atom Count:28
Complexity:503
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Extract from the above information

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Ruxolitinib Phosphate Tablets
Ingredients	The active ingredient of this product is ruxolitinib phosphate. Chemical name: (R)-3-(4-(7H-pyrrolo[2,3[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropionitrile phosphate Molecular formula: C17H18N6·H3PO4 Molecular weight: 404.36 Excipients of this product include lactose, microcrystalline cellulose, sodium starch glycolate, hydroxypropyl cellulose, povidone, colloidal silicon dioxide, magnesium stearate
Specifications	5mg*60s

Ruxolitinib Phosphate Tablets

Ingredients

The active ingredient of this product is ruxolitinib phosphate. Chemical name: (R)-3-(4-(7H-pyrrolo[2,3[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropionitrile phosphate Molecular formula: C17H18N6·H3PO4 Molecular weight: 404.36 Excipients of this product include lactose, microcrystalline cellulose, sodium starch glycolate, hydroxypropyl cellulose, povidone, colloidal silicon dioxide, magnesium stearate

Specifications

5mg*60s

Registered Holders

BIOPHORE INDIA PHARMACEUTICALS PVT LTD

United States
Active
MSN LABORATORIES PRIVATE LTD

United States
Active
ALIVUS LIFE SCIENCES LTD

United States
Active

See More Registered Holders

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