Raltegravir potassium
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MedKoo CAT#: 300210

CAS#: 871038-72-1 (potassium salt)

Description: Raltegravir, also known as MK-0518, is an antiretroviral drug used to treat HIV infection. Raltegravir is a human immunodeficiency virus (HIV) integrase strand transfer inhibitor (HIV-1 INSTI) with HIV-1 antiviral activity. Raltegravir binds to and inhibits integrase, an HIV enzyme that inserts viral genetic material into the genetic material of the infected human cell. Inhibition of integrase prevents insertion of HIV DNA into the human DNA genome, thus blocking HIV replication. It received approval by the U.S. Food and Drug Administration (FDA) in October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval.


Price and Availability

Size
Price

500mg
USD 150
5g
USD 850
50g
USD 3450
Size
Price

1g
USD 250
10g
USD 1450
100g
USD 4350
Size
Price

2g
USD 450
20g
USD 2150
200g
USD 5850

Raltegravir potassium, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 300210
Name: Raltegravir potassium
CAS#: 871038-72-1 (potassium salt)
Chemical Formula: C20H20FKN6O5
Exact Mass: 444.15575
Molecular Weight: 482.5137
Elemental Analysis: C, 49.79; H, 4.18; F, 3.94; K, 8.10; N, 17.42; O, 16.58


Synonym: MK0518; MK 0518; MK-0518; HSDB-8124; HSDB 8124; HSDB8124; Raltegravir; brand name: Isentress

IUPAC/Chemical Name: potassium 4-((4-fluorobenzyl)carbamoyl)-1-methyl-2-(2-(5-methyl-1,3,4-oxadiazole-2-carboxamido)propan-2-yl)-6-oxo-1,6-dihydropyrimidin-5-olate

SMILES Code: O=C(C(N=C(C(NC(C1=NN=C(C)O1)=O)(C)C)N2C)=C([O-])C2=O)NCC3=CC=C(F)C=C3.[K+]


Technical Data

Appearance:
solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO.

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

Related CAS#
518048-05-0 ( Raltegravir free);
871038-72-1 ( Raltegravir potassium salt)


References

  1: Calcagno A, D'Avolio A, Bonora S. Pharmacokinetic and pharmacodynamic evaluation of raltegravir and experience from clinical trials in HIV-positive patients. Expert Opin Drug Metab Toxicol. 2015 Jul;11(7):1167-76. doi: 10.1517/17425255.2015.1056732. Review. PubMed PMID: 26073580.

2: Ripamonti D, Benatti SV, Di Filippo E, Ravasio V, Rizzi M. Drug reaction with eosinophilia and systemic symptoms associated with raltegravir use: case report and review of the literature. AIDS. 2014 Apr 24;28(7):1077-9. doi: 10.1097/QAD.0000000000000204. Review. PubMed PMID: 24685746.

3: Liedtke MD, Tomlin CR, Lockhart SM, Miller MM, Rathbun RC. Long-term efficacy and safety of raltegravir in the management of HIV infection. Infect Drug Resist. 2014 Mar 18;7:73-84. doi: 10.2147/IDR.S40168. eCollection 2014. Review. PubMed PMID: 24672249; PubMed Central PMCID: PMC3965364.

4: Sharma M, Walmsley SL. Raltegravir as antiretroviral therapy in HIV/AIDS. Expert Opin Pharmacother. 2014 Feb;15(3):395-405. doi: 10.1517/14656566.2014.868884. Epub 2013 Dec 4. Review. PubMed PMID: 24304203.

5: Perry CM. Raltegravir: a review of its use in the management of HIV-1 infection in children and adolescents. Paediatr Drugs. 2014 Feb;16(1):91-100. doi: 10.1007/s40272-013-0058-9. Review. PubMed PMID: 24277175.

6: Karmon SL, Markowitz M. Next-generation integrase inhibitors : where to after raltegravir? Drugs. 2013 Mar;73(3):213-28. doi: 10.1007/s40265-013-0015-5. Review. PubMed PMID: 23413196.

7: Larson KB, King JR, Acosta EP. Raltegravir for HIV-1 infected children and adolescents: efficacy, safety, and pharmacokinetics. Adolesc Health Med Ther. 2013 Aug 27;4:79-87. doi: 10.2147/AHMT.S29462. eCollection 2013. Review. PubMed PMID: 24600298; PubMed Central PMCID: PMC3912854.

8: Mateo-Carrasco H, Gálvez-Contreras MC, Fernández-Ginés FD, Nguyen TV. Elevated liver enzymes resulting from an interaction between Raltegravir and Panax ginseng: a case report and brief review. Drug Metabol Drug Interact. 2012;27(3):171-5. doi: 10.1515/dmdi-2012-0019. Review. PubMed PMID: 23092794.

9: Shamroe CL, Bookstaver PB, Rokas KE, Weissman SB. Update on raltegravir and the development of new integrase strand transfer inhibitors. South Med J. 2012 Jul;105(7):370-8. doi: 10.1097/SMJ.0b013e318258c847. Review. PubMed PMID: 22766666.

10: Rokas KE, Bookstaver PB, Shamroe CL, Sutton SS, Millisor VE, Bryant JE, Weissman SB. Role of raltegravir in HIV-1 management. Ann Pharmacother. 2012 Apr;46(4):578-89. doi: 10.1345/aph.1Q616. Epub 2012 Apr 10. Review. PubMed PMID: 22496475.

11: Beare KD, Coster MJ, Rutledge PJ. Diketoacid inhibitors of HIV-1 integrase: from L-708,906 to raltegravir and beyond. Curr Med Chem. 2012;19(8):1177-92. Review. PubMed PMID: 22214459.

12: Chaudhary MA, Elbasha EH, Kumar RN, Nathanson EC. Cost-effectiveness of raltegravir in HIV/AIDS. Expert Rev Pharmacoecon Outcomes Res. 2011 Dec;11(6):627-39. doi: 10.1586/erp.11.79. Review. PubMed PMID: 22098278.

13: Nguyen BY, Isaacs RD, Teppler H, Leavitt RY, Sklar P, Iwamoto M, Wenning LA, Miller MD, Chen J, Kemp R, Xu W, Fromtling RA, Vacca JP, Young SD, Rowley M, Lower MW, Gottesdiener KM, Hazuda DJ. Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium. Ann N Y Acad Sci. 2011 Mar;1222:83-9. doi: 10.1111/j.1749-6632.2011.05972.x. Review. PubMed PMID: 21434946.

14: First-line raltegravir. No evidence of comparative effectiveness. Prescrire Int. 2010 Nov;19(110):248-50. Review. PubMed PMID: 21284354.

15: Brainard DM, Wenning LA, Stone JA, Wagner JA, Iwamoto M. Clinical pharmacology profile of raltegravir, an HIV-1 integrase strand transfer inhibitor. J Clin Pharmacol. 2011 Oct;51(10):1376-402. doi: 10.1177/0091270010387428. Epub 2011 Jan 5. Review. PubMed PMID: 21209233.

16: Delaugerre C. [Genetic barrier to antiretroviral drug-resistance. Focus on raltegravir, the first integrase inhibitor]. Med Mal Infect. 2010 Sep;40 Suppl 1:S1-10. doi: 10.1016/S0399-077X(10)70001-9. Review. French. PubMed PMID: 20800182.

17: Burger DM. Raltegravir: a review of its pharmacokinetics, pharmacology and clinical studies. Expert Opin Drug Metab Toxicol. 2010 Sep;6(9):1151-60. doi: 10.1517/17425255.2010.513383. Review. PubMed PMID: 20701552.

18: Clavel F. HIV resistance to raltegravir. Eur J Med Res. 2009 Nov 24;14 Suppl 3:47-54. Review. PubMed PMID: 19959417; PubMed Central PMCID: PMC3516824.

19: Johnson M. Raltegravir use in special populations. Eur J Med Res. 2009 Nov 24;14 Suppl 3:43-6. Review. PubMed PMID: 19959416; PubMed Central PMCID: PMC3516827.

20: Cossarini F, Castagna A, Lazzarin A. Raltegravir in treatment naive patients. Eur J Med Res. 2009 Nov 24;14 Suppl 3:22-9. Review. PubMed PMID: 19959413; PubMed Central PMCID: PMC3516825.