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Tofacitinib citrate

Tofacitinib citrate structure

CAS No:
540737-29-9
Formula:
C16H20N6O.C6H8O7
Chemical Name:
Tofacitinib citrate
Synonyms:
1-Piperidinepropanenitrile,4-methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-,(3R,4R)-,2-hydroxy-1,2,3-propanetricarboxylate (1:1);3-Piperidinamine,1-(cyanoacetyl)-4-methyl-N-methyl-N-1H-pyrrolo[2,3-d]pyrimidin-4-yl-,(3R,4R)-,2-hydroxy-1,2,3-propanetricarboxylate (1:1);Tasocitinib citrate;CP 690500-10;Tofacitinib citrate;CP 690550-10;Xeljanz;Xeljanz XR
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Description

Tofacitinib citrate is a JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively.

Tofacitinib citrate Basic Attributes

Molecular Weight：

504.497

Exact Mass：

504.196869

EC Number：

1592732-453-0

HScode：

29335990

Characteristics

PSA：

221

XLogP3：

0.23418

Appearance：

white to beige

Melting Point：

201 °C (decomp)

Water Solubility：

DMSO: soluble5mg/mL (clear solution; warmed)

Storage Conditions：

room temp

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

Precautionary statement(s)：

P201, P202, P264, P270, P281, P301+P312, P308+P313, P330, P405, P501

Hazard Statements：

H302

Tofacitinib citrate Use and Manufacturing

Tofacitinib (477600-75-2) API. Tofacitinib citrate combined with methotrexate is used to treat active rheumatoid arthritis with insufficient response to tumor necrosis factor inhibitors. Jak kinase inhibitor for the treatment of rheumatoid arthritis.

Drug Function and Efficacy

Tofacitinib is a Janus kinase (JAK) inhibitor that inhibits the activity of JAK1/JAK2, JAK1/JAK3 and JAK2/JAK2 combination enzymes, preventing the phosphorylation and activation of signal transducers and activators of transcription (STAT), thereby regulating intracellular activities and affecting the cellular hematopoietic process and cellular immune function.

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

Tofacitinib Citrate Tablets
Indication	Strong CYP3A4 Inhibitors Tofanib exposure is increased when coadministered with strong inhibitors of cytochrome P450 (CYP) 3A4 (e.g., ketoconazole) (see Dosage and Administration and Figure 5). Moderate CYP3A4 and Strong CYP2C19 Inhibitors Tofanib exposure is increased when coadministered with drugs that cause moderate CYP3A4 inhibition and strong CYP2C19 inhibition (e.g., fluconazole) (see Dosage and Administration and Figure 5). Strong CYP3A4 Inducers Tofanib exposure is decreased when coadministered with strong CYP3A4 inducers (e.g., rifampin) (see Dosage and Administration and Figure 5). Immunosuppressants There is a risk of increased immunosuppressive effects when Tofanib is coadministered with strong immunosuppressants (e.g., azathioprine, tacrolimus, cyclosporine). The coadministration of multiple doses of Tofanib with strong immunosuppressants has not been studied in rheumatoid arthritis. Tofanib is not recommended for use with biologic DMARDs or potent immunosuppressants (such as azathioprine and cyclosporine).
Specifications	5mg (based on tofacitinib)

Tofacitinib Citrate Tablets

Indication

Strong CYP3A4 Inhibitors Tofanib exposure is increased when coadministered with strong inhibitors of cytochrome P450 (CYP) 3A4 (e.g., ketoconazole) (see Dosage and Administration and Figure 5). Moderate CYP3A4 and Strong CYP2C19 Inhibitors Tofanib exposure is increased when coadministered with drugs that cause moderate CYP3A4 inhibition and strong CYP2C19 inhibition (e.g., fluconazole) (see Dosage and Administration and Figure 5). Strong CYP3A4 Inducers Tofanib exposure is decreased when coadministered with strong CYP3A4 inducers (e.g., rifampin) (see Dosage and Administration and Figure 5). Immunosuppressants There is a risk of increased immunosuppressive effects when Tofanib is coadministered with strong immunosuppressants (e.g., azathioprine, tacrolimus, cyclosporine). The coadministration of multiple doses of Tofanib with strong immunosuppressants has not been studied in rheumatoid arthritis. Tofanib is not recommended for use with biologic DMARDs or potent immunosuppressants (such as azathioprine and cyclosporine).

Specifications

5mg (based on tofacitinib)

Tofacitinib Citrate Extended Release Tablets
Ingredients	Active ingredient: Tofacitinib citrate. Chemical name: (3R,4R)-4-methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropionitrile citrate Molecular formula: C16H20N6O•C6H8O7 Molecular weight: 504.5 Excipients: sorbitol, sodium chloride, hydroxyethylcellulose, copovidone, magnesium stearate, cellulose acetate, hydroxypropylcellulose, film coating premix (gastric soluble)
Indication	Table 3 lists drugs with clinically important drug interactions when co-administered with XELJANZ and instructions for preventing or managing drug interactions. Table 3: Clinically relevant interactions affecting XELJANZ when co-administered with other drugs
Specifications	11mg14 tablets1 plate
Manufacturer	CSPC OUYI Pharmaceutical Co., Ltd.

Tofacitinib Citrate Tablets
Ingredients	Active ingredient: Tofacitinib citrate
Indication	Strong CYP3A4 inhibitors The exposure of tofacitinib is increased when tofacitinib is co-administered with strong cytochrome P450 (CYP) 3A4 inhibitors (such as ketoconazole) (see Dosage and Administration) (see instructions for details)
Specifications	5mg*28 tablets/box

Registered Holders

METROCHEM API PRIVATE LTD

United States
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AURORE LIFE SCIENCES PRIVATE LTD

United States
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MICRO LABS LTD

United States
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