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2017年10月18日星期三

Biggest Manufacturer ABT-530 [1353900-92-1] and Intermediates

ABT-530 [1353900-92-1]

Name: Pibrentasvir 
CAS#: 1353900-92-1 
Chemical Formula: C57H65F5N10O8

NMR, HPLC 99%+, LCMS, Stock more than 20G, pls kindly check:


ABT-530 Intermediate [CAS: 1890114-11-0],NMR, HPLC99%+, LCMS, COA, stock more than 1kg.





ABT-530 Intermediate [CAS: 1332357-14-8],NMR, HPLC99%+, LCMS, COA, stock more than 1kg.

ABT-530 Intermediate [CAS: 1292836-20-4],NMR, HPLC99%+, LCMS, COA, stock more than 1kg.


ABT-530 Intermediate [CAS: 1332356-31-6],NMR, HPLC99%+, LCMS, COA, stock more than 1kg.




Name:(2S,2'S)-2,2'-[[(2R,5R)-1-[3,5-Difluoro-4-[4-(4-fluorophenyl)-1-piperidinyl]phenyl]-2,5-pyrrolidinediyl]bis(6-fluoro-1H-benzimidazole-5,2-diyl)]bis-1-pyrrolidinecarboxylic acid 1,1'-bis(1,1-dimethylethyl) ester
CAS: 1890114-11-0, 
Molecular Formula: C53H59F5N8O4
Molecular Weight: 967.08
CAS Registry Number: 1890114-11-0


Description: Pibrentasvir, also known as ABT-530, is a protease inhibitor potentially for the treatment of HCV infection.


Name: Pibrentasvir  abt-530
CAS#: 1353900-92-1 
Chemical Formula: C57H65F5N10O8 
Exact Mass: 1112.4907 
Molecular Weight: 1113.2 
Elemental Analysis: C, 61.50; H, 5.89; F, 8.53; N, 12.58; O, 11.50

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
REFERENCES
1: Hussar DA, Inman B. Betrixaban, sofosbuvir/velpatasvir/voxilaprevir, and glecaprevir/pibrentasvir. J Am Pharm Assoc (2003). 2017 Nov - Dec;57(6):750-754. doi: 10.1016/j.japh.2017.10.002. PubMed PMID: 29092766.
2: Kaufman MB. Pharmaceutical Approval Update. P T. 2017 Nov;42(11):673-683. PubMed PMID: 29089721; PubMed Central PMCID: PMC5642154.
3: Kumada H, Watanabe T, Suzuki F, Ikeda K, Sato K, Toyoda H, Atsukawa M, Ido A, Takaki A, Enomoto N, Kato K, Alves K, Burroughs M, Redman R, Pugatch D, Pilot-Matias TJ, Krishnan P, Oberoi RK, Xie W, Chayama K. Efficacy and safety of glecaprevir/pibrentasvir in HCV-infected Japanese patients with prior DAA experience, severe renal impairment, or genotype 3 infection. J Gastroenterol. 2017 Oct 20. doi: 10.1007/s00535-017-1396-0. [Epub ahead of print] PubMed PMID: 29052790.
4: Gane E, Lawitz E, Pugatch D, Papatheodoridis G, Bräu N, Brown A, Pol S, Leroy V, Persico M, Moreno C, Colombo M, Yoshida EM, Nelson DR, Collins C, Lei Y, Kosloski M, Mensa FJ. Glecaprevir and Pibrentasvir in Patients with HCV and Severe Renal Impairment. N Engl J Med. 2017 Oct 12;377(15):1448-1455. doi: 10.1056/NEJMoa1704053. PubMed PMID: 29020583.
5: Asselah T, Kowdley KV, Zadeikis N, Wang S, Hassanein T, Horsmans Y, Colombo M, Calinas F, Aguilar H, de Ledinghen V, Mantry PS, Hezode C, Marinho RT, Agarwal K, Nevens F, Elkhashab M, Kort J, Liu R, Ng TI, Krishnan P, Lin CW, Mensa FJ. Efficacy of Glecaprevir/Pibrentasvir for 8 or 12 Weeks in Patients with HCV Genotype 2, 4, 5, or 6 Infection Without Cirrhosis. Clin Gastroenterol Hepatol. 2017 Sep 22. pii: S1542-3565(17)31162-X. doi: 10.1016/j.cgh.2017.09.027. [Epub ahead of print] PubMed PMID: 28951228.
6: Chayama K, Suzuki F, Karino Y, Kawakami Y, Sato K, Atarashi T, Naganuma A, Watanabe T, Eguchi Y, Yoshiji H, Seike M, Takei Y, Kato K, Alves K, Burroughs M, Redman R, Pugatch DL, Pilot-Matias TJ, Krishnan P, Oberoi RK, Xie W, Kumada H. Efficacy and safety of glecaprevir/pibrentasvir in Japanese patients with chronic genotype 1 hepatitis C virus infection with and without cirrhosis. J Gastroenterol. 2017 Sep 25. doi: 10.1007/s00535-017-1391-5. [Epub ahead of print] PubMed PMID: 28948366.
7: Lamb YN. Glecaprevir/Pibrentasvir: First Global Approval. Drugs. 2017 Oct;77(16):1797-1804. doi: 10.1007/s40265-017-0817-y. PubMed PMID: 28929412.
8: Wyles D, Poordad F, Wang S, Alric L, Felizarta F, Kwo PY, Maliakkal B, Agarwal K, Hassanein T, Weilert F, Lee SS, Kort J, Lovell SS, Liu R, Lin CW, Pilot-Matias T, Krishnan P, Mensa FJ. Glecaprevir/Pibrentasvir for HCV Genotype 3 Patients with Cirrhosis and/or Prior Treatment Experience: A Partially Randomized Phase III Clinical Trial. Hepatology. 2017 Sep 19. doi: 10.1002/hep.29541. [Epub ahead of print] PubMed PMID: 28926120.
9: Davis MI, Chute DF, Chung RT, Sise ME. When and how can nephrologists treat hepatitis C virus infection in dialysis patients? Semin Dial. 2017 Sep 18. doi: 10.1111/sdi.12650. [Epub ahead of print] Review. PubMed PMID: 28925068.
10: Toyoda H, Chayama K, Suzuki F, Sato K, Atarashi T, Watanabe T, Atsukawa M, Naganuma A, Notsumata K, Osaki Y, Nakamuta M, Takaguchi K, Saito S, Kato K, Pugatch D, Burroughs M, Redman R, Alves K, Pilot-Matias TJ, Oberoi RK, Fu B, Kumada H. Efficacy and Safety of Glecaprevir/Pibrentasvir in Japanese Patients with Chronic Genotype 2 Hepatitis C Virus Infection. Hepatology. 2017 Sep 2. doi: 10.1002/hep.29510. [Epub ahead of print] PubMed PMID: 28865152.
11: Forns X, Lee SS, Valdes J, Lens S, Ghalib R, Aguilar H, Felizarta F, Hassanein T, Hinrichsen H, Rincon D, Morillas R, Zeuzem S, Horsmans Y, Nelson DR, Yu Y, Krishnan P, Lin CW, Kort JJ, Mensa FJ. Glecaprevir plus pibrentasvir for chronic hepatitis C virus genotype 1, 2, 4, 5, or 6 infection in adults with compensated cirrhosis (EXPEDITION-1): a single-arm, open-label, multicentre phase 3 trial. Lancet Infect Dis. 2017 Oct;17(10):1062-1068. doi: 10.1016/S1473-3099(17)30496-6. Epub 2017 Aug 14. PubMed PMID: 28818546.
12: Kosloski MP, Zhao W, Asatryan A, Kort J, Geoffroy P, Liu W. No Clinically Relevant Drug-Drug Interactions between Methadone or Buprenorphine-Naloxone and Antiviral Combination Glecaprevir and Pibrentasvir. Antimicrob Agents Chemother. 2017 Sep 22;61(10). pii: e00958-17. doi: 10.1128/AAC.00958-17. Print 2017 Oct. PubMed PMID: 28807904; PubMed Central PMCID: PMC5610490.
13: Lin CW, Dutta S, Ding B, Wang T, Zadeikis N, Asatryan A, Kort J, Campbell A, Podsadecki T, Liu W. Pharmacokinetics, Safety, and Tolerability of Glecaprevir and Pibrentasvir in Healthy White, Chinese, and Japanese Adult Subjects. J Clin Pharmacol. 2017 Dec;57(12):1616-1624. doi: 10.1002/jcph.959. Epub 2017 Aug 11. PubMed PMID: 28800195.
14: Lin CW, Dutta S, Zhao W, Asatryan A, Campbell A, Liu W. Pharmacokinetic Interactions and Safety of Coadministration of Glecaprevir and Pibrentasvir in Healthy Volunteers. Eur J Drug Metab Pharmacokinet. 2017 Jul 7. doi: 10.1007/s13318-017-0428-8. [Epub ahead of print] PubMed PMID: 28688001.
15: Soriano V, Fernandez-Montero JV, de Mendoza C, Benitez-Gutierrez L, Peña JM, Arias A, Barreiro P. Treatment of hepatitis C with new fixed dose combinations. Expert Opin Pharmacother. 2017 Aug;18(12):1235-1242. doi: 10.1080/14656566.2017.1346609. Epub 2017 Jul 30. Review. PubMed PMID: 28644739.
16: Molino S, Martin MT. Hepatitis C Virus Resistance Testing in Genotype 1: The Changing Role in Clinical Utility. Ann Pharmacother. 2017 Sep;51(9):811-816. doi: 10.1177/1060028017704857. Epub 2017 May 6. PubMed PMID: 28480743.
17: Lin CW, Dutta S, Asatryan A, Wang H, Clifton J 2nd, Campbell A, Liu W. Pharmacokinetics, Safety, and Tolerability Following Single and Multiple Doses of Pibrentasvir in a First-in-Human Study. Clin Pharmacol Drug Dev. 2017 May 2. doi: 10.1002/cpdd.350. [Epub ahead of print] PubMed PMID: 28464496.
18: Kwo PY, Poordad F, Asatryan A, Wang S, Wyles DL, Hassanein T, Felizarta F, Sulkowski MS, Gane E, Maliakkal B, Overcash JS, Gordon SC, Muir AJ, Aguilar H, Agarwal K, Dore GJ, Lin CW, Liu R, Lovell SS, Ng TI, Kort J, Mensa FJ. Glecaprevir and pibrentasvir yield high response rates in patients with HCV genotype 1-6 without cirrhosis. J Hepatol. 2017 Aug;67(2):263-271. doi: 10.1016/j.jhep.2017.03.039. Epub 2017 Apr 13. PubMed PMID: 28412293.
19: Ng TI, Krishnan P, Pilot-Matias T, Kati W, Schnell G, Beyer J, Reisch T, Lu L, Dekhtyar T, Irvin M, Tripathi R, Maring C, Randolph JT, Wagner R, Collins C. In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS5A Inhibitor Pibrentasvir. Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02558-16. doi: 10.1128/AAC.02558-16. Print 2017 May. PubMed PMID: 28193664; PubMed Central PMCID: PMC5404558.
20: Poordad F, Felizarta F, Asatryan A, Sulkowski MS, Reindollar RW, Landis CS, Gordon SC, Flamm SL, Fried MW, Bernstein DE, Lin CW, Liu R, Lovell SS, Ng TI, Kort J, Mensa FJ. Glecaprevir and pibrentasvir for 12 weeks for hepatitis C virus genotype 1 infection and prior direct-acting antiviral treatment. Hepatology. 2017 Aug;66(2):389-397. doi: 10.1002/hep.29081. Epub 2017 Apr 10. PubMed PMID: 28128852; PubMed Central PMCID: PMC5573922.





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