Patent of Fresenius Kabi Oncology Ltd.Novel intermediates and process for the preparation of lapatinib and…….

New Drug Approvals



Title: Lapatinib
CAS Registry Number: 231277-92-2
CAS Name:N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine
Manufacturers’ Codes: GW-572016
Trademarks: Tykerb (GSK)
Molecular Formula: C29H26ClFN4O4S
Molecular Weight: 581.06
Percent Composition: C 59.94%, H 4.51%, Cl 6.10%, F 3.27%, N 9.64%, O 11.01%, S 5.52%

Lapatinib (INN), used in the form of lapatinib ditosylate, (USAN) (Tykerb/Tyverb, GSK) is an orally active drug for breast cancer and other solid tumours. It is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways. It is used in combination therapy for HER2-positive breast cancer. It is used for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 (ErbB2).


Beilstein J. Org. Chem.2013,9, 2265–2319.

GlaxoSmithKline’s lapatinib (3.38, Tykerb) is a novel dual kinase inhibitor used in the treatment of solid tumors…

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Lilly Terminates Phase II study for LY2886721, a Beta Secretase Inhibitor for the Treatment for Alzheimer’s Disease

June 14 2013 | By Márcio Barra

Eli Lilly released yesterday a press release were it stated it decided to discontinue a phase II study for an Alzheimer’s disease medicine, after concerns over patients safety.

The medicine in question, LY2886721 a beta-secretase (BACE) inhibitor, was being investigated as a once daily treatment for Alzheimer’s disease. Beta-secretase is a major protease in the processing of amyloid precursor protein leading to the production of amyloid-β. It is assumed an excess level of amyloid-β in the brain over a long time period is a leading factor in the pathogenesis of Alzheimer’s Disease, and as such it is one of the leading treatment hypothesis, alongside Tau protein, despite Bapineuzumab’s 2012 failure.

The decision to terminate the phase II study was due to abnormal liver biochemical tests in patients. In the press release, Lilly states it believes that the abnormal liver biochemical tests observed in the study…

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Parabens … Is It Bad For You?


PP Paraben

What are parabens?

  • Most widely used preservatives in cosmetic products.
  • Chemically, parabens are esters of p-hydroxybenzoic acid.
  • Can be found naturally in blueberries.

Why are preservatives used in cosmetics?

  • To protect them against microbial growth, both to protect consumers and to maintain product integrity.
  • To extend the shelf life of just about every packaged beauty product.

What kinds of products contain parabens?

  • Parabens are used in a wide variety of cosmetics, as well as foods and drugs.
  • Cosmetics that may contain parabens include deodorants, antiperspirants, makeup, moisturizers, toothpaste, hair care products, and shaving products, among others.

What are some of the retail names for parabens?

  • Parabens are usually easy to identify by name – just look for a ‘paraben’ attached at the back. Eg. methylparaben, propylparaben, butylparaben, benzylparaben, ethylparaben or isobutylparaben.

Why are parabens controversial?

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Drug development can be a gas

New Drug Approvals

Pharmaceutical and biotech industries are heavily dependent on gas mixtures to grow biological cultures

The pharmaceutical and biotech industries rely heavily on industrial gases for applications such as supercritical fluid chromatgraphy and lyophilisation. Gas supply systems theefore need to offer high purity and traceability through the supply chain

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Ayurveda Herbs : Medicinal uses of Turmeric

New Drug Approvals



Curcumin keto form
Curcumin enol form

Turmeric contains up to 5% essential oils and curcumin of about three percent by weight, a polyphenol. Curcumin is the active substance of turmeric and curcumin is known as C.I. 75300, or Natural Yellow 3. The systematic chemical name is (1E,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione.

It can exist at least in two tautomeric forms, keto and enol. Curcumin is a pH indicator. In acidic solutions (pH <7.4) it turns yellow, whereas in basic (pH > 8.6) solutions it turns bright red.

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