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Tofacitinib



Chemical Properties of 'Tofacitinib'

CAT No. :

CS-O-10853
CAS Registry No. : 477600-75-2
Category : API Standards
Molecular Weight: 312.37
Molecular Formula : C₁₆H₂₀N₆O



OTHER INFORMATION of 'Tofacitinib'
Purity : Not less than 95%
Therapeutic : Anti-Cancer / Oncology
Purity : Not less than 95%
Therapeutic : Anti-Cancer / Oncology
IUPAC Name :3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
Applicationnotes :"CP-690550 is a pyrrolo[2,3-d]pyrimidine derivative, as Janus kinase inhibitor for treatment of rheumatoid arthritis"
Synonym :Not Available
References :"Sheiner, L,, et al,: Clin, Pharmacol, Ther,, 25, 358 (1979),"
Smileys :CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N
Appearance :White to off white solid
Color / Form :Yellow foam
Melting Point :White crystalline solid. MP: 199-206 °C /Tofacitinib monocitrate/
Solubility :In water, 155.1 mg/L at 25 °C (est)
Use Classification :Human Drugs -> EU pediatric investigation plans
Hazard Class :Acute Tox. 4 (25%)
EC Number :689-145-4
UNII :87LA6FU830
NCI Thesaurus Code :C95800
RXCUI :1357536
MeSH Entry Terms :CP 690,550
Other Synonyms :Tofacitinib
Removed Synonyms :Xeljanz
Vapor Pressure : 1.32X10-10 mm Hg at 25 °C (est)
Other Experimental Properties :Hydroxyl radical reaction rate constant = 2.57X10-10 cu cm/molec-sec at 25 °C (est)
Disposal Methods :SRP: Expired or waste pharmaceuticals shall carefully take into consideration applicable DEA, EPA, and FDA regulations. It is not appropriate to dispose by flushing the pharmaceutical down the toilet or discarding to trash. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.
Toxicity Summary :Minimum lethal dose in rat: 500 mg/kg. Maximum asymptomatic dose in non human primate: 40 mg/kg. Lymphatic, immune system, bone marrow and erythroid cell toxicity was seen in animal studies involving rate and monkeys. Doses used in these studies ranged from 1mg/kg/day to 10mg/kg/day, over a duration of 6 weeks to 6 months. Lymphopenia, neutropenia, and anemia is seen in human subjects and may call for an interruption or discontinuation of therapy if severe. Reduced female fertility in rats was seen at exposures 17 times the maximum recommended human dose. Fertility may be impaired in human females and harm may be caused to unborn child. Carcinogenic potential is seen, however evidence for dose dependency is lacking. Because the janus kinase pathway plays a role in stimulating the production of red blood cells and is involved in immune cell function, inhibition of this pathway leads to increased risk of anemia, neutropenia, lymphopenia, cancer and infection. Lymphopenia, neutropenia, and anemia in human subjects may call for an interruption or discontinuation of therapy if severe. Role of JAK inhibition in the development of gastrointestinal perforation is not known.
Hepatotoxicity :In the large registration clinical trials, serum aminotransferase elevations occurred in 28% to 34% of tofacitinib treated subjects compared to 25% in comparator arms and 10% in placebo recipients. These elevations were typically mild and transient, but values above 3 times the upper limit of normal (ULN) occurred in 1% to 2% of patients on tofacitinib compared to less than 1% on placebo. The elevations occasionally led to early discontinuations, but more often resolved even without dose adjustment. In prelicensure studies, there were no instances of clinically apparent liver injury attributed to tofacitinib. Since approval and more wide scale availability of tofacitinib, there have been no published reports of hepatotoxicity associated with its use but a proportion of patients do develop serum aminotransferase elevations which in some cases leads to drug discontinuation. While other Janus kinase inhibitors such as ruxolitinib have been associated with episodes of reactivation of hepatitis B, spontaneous reports of clinically apparent reactivation of hepatitis during tofacitinib therapy have not been reported. On the other hand, retrospective studies on patients with HBsAg and inactive liver disease who were treated with tofacitinib have been reported to develop rising levels of HBV DNA and modest elevations in serum aminotransferase levels without symptoms. In contrast, studies of patients with anti-HBc without HBsAg in serum have shown no evidence of HBV DNA rises and appearance of HBsAg. Thus, reactivation of hepatitis B during therapy can occur, although it is generally mild and self-limited in course. Whether reactivation of hepatitis B can arise after therapy of susceptible patients with tofacitinib for severe COVID-19 pneumonia is unknown, but there have been no such reports to date.
Interactions :In healthy individuals, the CYP3A inducer rifampin (600 mg orally once daily for 7 days) decreased peak plasma concentrations and AUC of tofacitinib (single oral dose of 30 mg) by 74 and 84%, respectively. Concomitant use of rifampin may decrease efficacy of tofacitinib.
Antidoteand Emergency Treatment :/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/
Human Toxicity Excerpts :/CASE REPORTS/ Tofacitinib is a novel drug that inhibits the JAK-STAT signaling pathway. It has been approved for the treatment of psoriatic arthritis and it is under investigation for the treatment of psoriasis and other inflammatory disorders. We report a case of pulmonary cryptococcosis in an otherwise immunocompetent patient taking tofacitinib for psoriasis. We hypothesized that tofacitinib contributed to this infection through inhibition of cytokines required for differentiation of T cells and suppression of macrophage activation. As dermatologists begin to use this drug they should be aware of the potential for cryptococcocal infection, because delay of diagnosis may increase the risk of a life-threatening outcome.
Non Human Toxicity Excerpts :/LABORATORY ANIMALS: Acute Exposure/ In cynomolgus monkeys emesis and decreased activity were observed at single oral doses of >/= 200 mg/kg (divided 3 times daily [TID] approximately 7 hours apart).
Protein Binding :40%, mostly bound to albumin.
Exact Mass :312.16985928
InChI :InChI=1S/C16H20N6O/c1-11-5-8-22(14(23)3-6-17)9-13(11)21(2)16-12-4-7-18-15(12)19-10-20-16/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20)/t11-,13+/m1/s1
InchIKey :UJLAWZDWDVHWOW-YPMHNXCESA-N
Canonical SMILES :CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N
Isomeric SMILES :C[C@@H]1CCN(C[C@@H]1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N
Product Description :Tofacitinib is a pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor and an antirheumatic drug. It is a pyrrolopyrimidine, a N-acylpiperidine, a nitrile and a tertiary amino compound.
Custom Duty : Applicable
Port of Loading : Canada
Expected Dispatch : 15-Aug-2022
Taxes : Not Applicable
Refund Policy : 30-days money back
Custom Duty : Applicable
Port of Loading : Canada
Expected Dispatch : 15-Aug-2022
Taxes : Not Applicable
Refund Policy : 30-days money back


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