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Fosravuconazole L-lysine ethanolate, ホスラブコナゾール L-リシンエタノール付加物

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Image result for Fosravuconazole L-lysine ethanolate

Image result for Fosravuconazole L-lysine ethanolate

C23H20F2N5O5PS▪C6H14N2O2▪C2H6O : 739.73
[914361-45-8]

[(2R,3R)-3-[4-(4-cyanophenyl)-1,3-thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1,2,4-triazol-1-yl)butan-2-yl]oxymethyl dihydrogen phosphate;(2S)-2,6-diaminohexanoic acid;ethanol

L-Lysine [[(2R,3R)-3-[4-(4-cyanophenyl)-1,3-thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butan-2-yl]oxy]methyl dihydrogen phosphate ethanol

BFE-1224
BMS-379224
E-1224

ravuconazole prodrugs, ravuconazole methyl phosphate

fosravuconazole bis(L-lysine)

ホスラブコナゾール L-リシンエタノール付加物

Formula
C23H20F2N5O5PS. C6H14N2O2. C2H6O
CAS
914361-45-8
Mol weight
739.727

Antifungal, Ergosterol biosynthesis inhibitor

Fungal infection; Onychomycosis; Trypanosoma cruzi infection

PMDA JAPAN APPROVED

2018/1/19 PMDA APPROVED Fosravuconazole L-lysine ethanolate Nailin Sato Pharmaceutical

FOR

Tinea, nail (onychomycosis)

NOTE THIS STR

Image result for fosravuconazole

  • 4-[2-[(1R,2R)-2-(2,4-Difluorophenyl)-1-methyl-2-[(phosphonooxy)methoxy]-3-(1H-1,2,4-triazol-1-yl)propyl]-4-thiazolyl]benzonitrile
  • E 1224
  • Fosravuconazole
  • CAS  351227-64-0

Drugs for Neglected Diseases initiative (DNDi), under license from Eisai, is developing fosravuconazole for CD  and eumycetoma 

In February 2013, the drug was in phase II/III development by Seren Pharmaceuticals for onychomycosis in North America, Europe and Asia, including Japan,

In 2010, the product was licensed exclusively to Brain Factory (now Seren Pharma) for development, commercialization and sublicense in Japan for the treatment of fungal infections. In 2014, Seren Pharma signed an agreement with Sato Pharma, granting them the development and commercialization rights of the product in Japan

Sato Pharmaceutical Co., Ltd. has obtained marketing and manufacturing approval for the oral antifungal agent, Nailin capsules 100mg containing the active ingredient fosravuconazole L-lysine ethanolate (fosravuconazole) for the treatment of onychomycosis in Japan.

Sato Pharma conducted a phase III clinical study of the agent in patients with onychomycosis in Japan, and after confirming efficacy and safety of the agent in the study, the company applied for marketing and manufacturing authorization in January 2017.

Fosravuconazole, the active ingredient of Nailin capsules 100mg, is a new triazole class oral antifungal component discovered by Eisai.

Fosravuconazole, the active ingredient of Nailin capsules 100mg, is a new triazole class oral antifungal component discovered by Eisai. By providing Nailin capsules 100mg as a new option for the treatment of onychomycosis, Sato Pharma and Eisai will strive to fulfil the needs of onychomycosis patients and healthcare professionals.

Onychomycosis is a fungal infection of the toenails or fingernails that may involve any component of the nail unit, including the matrix, bed, or plate. With Sato Pharma now having obtained marketing and manufacturing approval for Nailin capsules 100mg, as an oral treatment for onychomycosis, this is the first new treatment for the disease in approximately 20 years.

Fosravuconazole is a prodrug of ravuconazole originated by Eisai. In 2018, the product was approved in Japan for the treatment of onychomycosis. Fosravuconazole is being tested in phase II clinical studies at Eisai and Drugs for Neglected Diseases Initiative (DNDi) for the treatment of american trypanosomiasis (Chagas disease)

Image result for Fosravuconazole L-lysine ethanolate WIKI

Onychomycosis due to Trichophyton rubrum, right and left great toe. Tinea unguium.
Image/CDC

Sato Pharmaceutical Co., Ltd. obtained marketing and manufacturing approval for the oral antifungal agent NAILIN Capsules 100mg containing the active ingredient fosravuconazole L-lysine ethanolate (fosravuconazole) for the treatment of onychomycosis in Japan on January 19, 2018.
Fosravuconazole, the active ingredient of NAILIN Capsules 100mg, is a new triazole class oral antifungal component discovered by Eisai. Sato Pharma conducted a Phase III clinical study of the agent in patients with onychomycosis in Japan, and after confirming efficacy and safety of the agent in the study, Sato Pharma applied for marketing and manufacturing authorization in January 2017.Sato Pharma and Eisai Co., Ltd. are jointly providing information on its proper use.

Onychomycosis is a fungal infection of the toenails or fingernails that may involve any component of the nail unit, including the matrix, bed, or plate.

Onychomycosis affects 1 in every 10 Japanese people, and there are an estimated approximately 11 million sufferers in Japan. With Sato Pharma now having obtained marketing and manufacturing approval for NAILIN Capsules 100mg, as an oral treatment for onychomycosis, this is the first new treatment for the disease in approximately 20 years.

Image result for Onychomycosis

Sato Pharmaceutical Co. Ltd., Eisai Co. Ltd., and Seren Pharmaceuticals Inc. announced that Sato Pharma and Eisai will co-promote a new triazole class oral antifungal agent (development code: BFE1224) containing the active ingredient fosravuconazole L-lysine ethanolate (fosravuconazole) in Japan, based on an agreement between the three companies. The agent is currently under regulatory review for the treatment of onychomycosis.

After receiving regulatory approval, Sato Pharma will begin distributing the agent, and Sato Pharma and Eisai will jointly provide information on its proper use.

Fosravuconazole is a new oral antifungal component developed by Eisai. In 2010, Eisai concluded a license agreement with Seren Pharma (formerly known as Brain Factory Co., Ltd.), granting them exclusive rights to develop, commercialize, and sublicense the agent in Japan.

In 2014, Seren Pharma concluded an agreement with Sato Pharma, granting them the development and commercialization rights, and both companies continued to develop the agent for treating onychomycosis. In January 2017, Sato Pharma applied for marketing authorization for the agent.

Sato Pharma, Eisai, and Serena Pharma will cooperate to maximize the value of fosravuconazole in order to fulfil the unmet medical needs of patients with fungal diseases.

Courtesy- techno.bigmir

PATENT

WO 2006118351

Journal of the American Chemical Society, 139(31), 10733-10741; 2017

PAPER

BMS-379224, a water-soluble prodrug of ravuconazole
42nd Intersci Conf Antimicrob Agents Chemother (ICAAC) (September 27-30, San Diego) 2002, Abst F-817

PATENT

WO 2006118351

WO 2007072851

WO 2001052852

WO 2006026274

WO 2013082102

WO 2013157584

////////////ホスラブコナゾール L-リシンエタノール付加物, Fosravuconazole L-lysine ethanolate, Nailin, SATO, BFE-1224, BMS-379224, E-1224, JAPAN 2018, ravuconazole prodrugs, ravuconazole methyl phosphate, fosravuconazole bis(L-lysine), Drugs for Neglected Diseases initiative, DNDi

CCO.CC(C1=NC(=CS1)C2=CC=C(C=C2)C#N)C(CN3C=NC=N3)(C4=C(C=C(C=C4)F)F)OCOP(=O)(O)O.C(CCN)CC(C(=O)O)N

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DR ANTHONY CRASTO

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 30 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, Dr T.V. Radhakrishnan and Dr B. K. Kulkarni, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 30 year tenure till date Dec 2017, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 50 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 19 lakh plus views on New Drug Approvals Blog in 216 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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