NEW DRUGS – Page 5 – All About Drugs

FDA Lifts Clinical Hold on Canada company Cangene’s Hemophilia Compound

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Jul 312013

FDA lifts clinical hold on Cangene’s hemophilia compound IB1001

WINNIPEG, July 29, 2013 /CNW/ – Cangene Corporation (Cangene) today announces that the U.S. Food and Drug Administration (FDA) has lifted the clinical hold previously placed on clinical trials evaluating the safety and efficacy of IB1001, a recombinant Factor IX (rFIX) product being developed for the treatment and prevention of bleeding episodes with hemophilia B.

http://www.pharmalive.com/fda-lifts-clinical-hold-on-cangenes-hemophilia-compoun

IB1001 is an intravenous recombinant Factor IX (rFIX) being developed for the treatment and prevention of bleeding episodes in people with hemophilia B. The IB1001 development program includes a comprehensive set of pharmacokinetic, safety, and efficacy data from a Phase 3 clinical trial in people affected by hemophilia B, including a surgery sub-study.

A biologics license application (BLA) was submitted to the U.S. Food and Drug Administration (FDA) in March 2012 and a Marketing Authorization Application (MAA) was submitted to the European Medicines Agency (EMA) in October 2011.

In July 2012, IB1001 was put on a clinical hold by the FDA due to a higher than expected rate of host cell antibody development in people treated with IB1001.

Cangene Corporation (TSX: CNJ) has completed its previously announced acquisition of the worldwide rights to investigational hemophilia compound IB1001 (recombinant FIX), as well as Inspiration’s rights to two product candidates in pre-clinical development: IB1007 (recombinant FVIIa) and IB1008 (recombinant FVIII) from Ipsen (Euronext: IPN; ADR: IPSEY) and Inspiration Biopharmaceuticals, Inc., in connection with Inspiration’s bankruptcy proceedings.

The transaction was slated to close on February 15, 2013.

Pursuant to the terms of the agreement, Cangene will pay approximately US $5.9 million upfront and up to $50 million in potential additional commercial milestones as well net sales payments equivalent to tiered double-digit percentage of IB1001 annual net sales.

http://canadianprivateequity.com/cangene-closes-56-million-acquisition-of-inspirations-ib1001-hemophilia-b-product/2013/02/20/

amcrasto@gmail.com

Perrigo Buying Elan For $8.6B

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Jul 302013

U.S. drugmaker Perrigo agreed to buy Ireland’s Elan for $8.6 billion in a deal that should allow the rapidly growing company to reduce its tax bill and boost its royalty stream.

Perrigo Co. said it would pay Elan Corp.’s investors $6.25 per share in cash and $10.25 in Perrigo stock, an 11% premium over Elan’s closing price on July 26. Elan shares in Dublin surged 13% higher to 12.58 euros ($16.71), above Perrigo’s offer price, following news of the takeover.

http://www.dddmag.com/news/2013/07/perrigo-buying-elan-86b

Indian biopharma giant Biocon clocks revenue worth $121 mn

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Jul 302013

Kiran Mazumdar-Shaw, chairman and managing director, Biocon.

Indian biopharma giant Biocon reported healthy growth of 22 percent for Q1 FY14 riding on the back of an increased geographical footprint in the emerging markets

Bangalore: Indian biopharma giant Biocon reported healthy growth of 22 percent for Q1 FY14. The firm clocked revenues worth $121 million (Rs723 crore), EBITDA of $29.50 million (Rs175 crore); and profit after tax (PAT) of $15.80 million (Rs94 crore).

Biocon’s India-focused branded formulations vertical as well as research services continue to grow at a steady pace

B Family Album -Structural Biology: First structures of class B G protein-coupled receptors may aid drug hunts

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Jul 292013

Two new G-Protein Coupled Receptor structures, the glucagon receptor (computer model with extracellular domain) and corticotropin-releasing factor receptor, showing their location on the GPCR family tree.

A computer model of a full-length glucagon receptor (left) and a crystal structure of a corticotropin-releasing factor receptor (right) add details of class B receptors to the class A structures already on the GPCR family tree.

Credit: Katya Kadyshevskaya

As many as 30% of drugs on the market target G protein-coupled receptors (GPCRs), a family of signaling conduits that snake back and forth across cell membranes. But there are several classes of these proteins, and scientists’ knowledge of the structures is almost entirely restricted to just one, the class A subtype. So drugs could be missing a lot of targets. Aim could improve, however, now that researchers have the first two reports of class B GPCR structures (Nature 2013, DOI: 10.1038/nature12357 and10.1038/nature12393

read all at

http://cen.acs.org/articles/91/i30/B-Family-Album.html

AstraZeneca: FDA-RESUBMISSION OF THE NDA FOR DAPAGLIFLOZIN FOR THE TREATMENT OF TYPE 2 DIABETES

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Jul 272013

DAPAGLIFLOZIN

AstraZeneca and Bristol-Myers Squibb Company today announced that the U.S. Food and Drug Administration (FDA) has acknowledged receipt of the New Drug Application (NDA) resubmission for investigational drug dapagliflozin for the treatment of adults with type 2 diabetes. The FDA assigned a new Prescription Drug User Fee Act goal date of January 11 2014.

The dapagliflozin Phase II/III clinical development program included more than 12,000 adult patients with diabetes (more than 8,000 patients received dapagliflozin) in 26 clinical trials. In response to the FDA’s January 2012 complete response letter requesting additional data to allow a better assessment of the benefit-risk profile of dapagliflozin, the NDA resubmission includes several new studies and additional long-term data (up to four years’ duration) from previously submitted studies, resulting in an overall increase in patient-years exposure to dapagliflozin of more than 50 percent.

Dapagliflozin, an investigational compound, is a selective and reversible inhibitor of sodium-glucose cotransporter 2 (SGLT2), which works independently of insulin. It is currently approved for the treatment of type 2diabetes in the European Union, Australia, Brazil, Mexico and New Zealand

READ ALL AT

http://www.swedishwire.com/press-releases/17843-astrazeneca-fda-acknowledges-receipt-of-resubmission-of-the-new-drug-application-for-investigational-compound-dapagliflozin-for-the-treatment-of-type-2-diabetes

Health Canada approves two GSK drugs for metastatic melanoma

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Jul 262013

Health Canada has approved two GlaxoSmithKline (GSK) drugs, Tafinlar(TM) (dabrafenib mesilate) and Mekinist(TM) (trametinib), for patients with unresectable or metastatic melanoma. Dabrafenib mesylate, which is a BRAF-inhibitor, is indicated as a monotherapy oral treatment for unresectable melanoma or metastatic melanoma in adult …http://www.gsk.ca/english/html/media-centre/2013-07-24.html

Iron Oxide Nanoparticles Show the Way

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Jul 262013

Iron oxide nanoparticles precisely direct stem cells to damage tissues, thereby increasing their therapeutic potential

http://www.chemistryviews.org/details/news/5039301/Iron_Oxide_Nanoparticles_Show_the_Way.html

Probiotic Could Prevent Kidney Stones

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Jul 252013

The discovery of a gene’s function in E. coli and other bacteria might lead to a probiotic to prevent calcium-oxalate urinary stones, the most common type of kidney stone. Human cells can’t metabolize oxalate and high concentrations can result in painful blockages of the urinary tract.

http://www.dddmag.com/news/2013/07/probiotic-could-prevent-kidney-stones?et_cid=3386057&et_rid=523035093&type=cta

http://www.precisionnutrition.com/all-about-kidney-stones

AstraZeneca began a pivotal trial with selumetinib , thyroid cancer, Phase 3 trial

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Jul 232013

selumetinib

Array Biopharma To Report Top-line Results From ARRY-502 Asthma Trial
Sacramento Bee
AstraZeneca began a pivotal trial with selumetinib (an Array-invented drug) in patients with thyroid cancer in May 2013 and expects to begin a Phase 3 trial in patients with non-small cell lung cancer during the second half of 2013. Three other Array …

http://www.sacbee.com/2013/07/22/5586413/array-biopharma-to-report-top.html

Selumetinib (AZD6244) is a drug being investigated for the treatment of various types of cancer, for example non-small cell lung cancer (NSCLC).

The gene BRAF is part of the MAPK/ERK pathway, a chain of proteins in cells that communicates input from growth factors. Activating mutations in the BRAF gene, primarily V600E (meaning that the amino acid valine in position 600 is replaced by glutamic acid), are associated with lower survival rates in patients with papillary thyroid cancer. Another type of mutation that leads to undue activation of this pathway occurs in the gene KRAS and is found in NSCLC. A possibility of reducing the activity of the MAPK/ERK pathway is to block the enzyme MAPK kinase (MEK), immediately downstream of BRAF, with the drug selumetinib. More specifically, selumetinib blocks the subtypes MEK1 and MEK2 of this enzyme.^[1]

In addition to thyroid cancer, BRAF-activating mutations are prevalent in melanoma (up to 59%), colorectal cancer (5–22%), serous ovarian cancer (up to 30%), and several other tumor types.^[2]

KRAS mutations appear in 20 to 30% of NSCLC cases and about 40% of colorectal cancer.^[1]

A Phase II clinical trial about selumetinib in NSCLC has been completed in September 2011;^[3] one about cancers with BRAF mutations is ongoing as of June 2012^[update].^[4]

Troiani, T.; Vecchione, L.; Martinelli, E.; Capasso, A.; Costantino, S.; Ciuffreda, L. P.; Morgillo, F.; Vitagliano, D. et al. (2012). “Intrinsic resistance to selumetinib, a selective inhibitor of MEK1/2, by cAMP-dependent protein kinase a activation in human lung and colorectal cancer cells”. British Journal of Cancer 106 (10): 1648–1659. doi:10.1038/bjc.2012.129. PMC 3349172. PMID 22569000. |displayauthors= suggested (help) edit
Davies, H.; Bignell, G. R.; Cox, C.; Stephens, P.; Edkins, S.; Clegg, S.; Teague, J.; Woffendin, H. et al. (2002). “Mutations of the BRAF gene in human cancer”. Nature 417 (6892): 949–954. doi:10.1038/nature00766. PMID 12068308. |displayauthors= suggested (help) edit
ClinicalTrials.gov NCT00890825 Comparison of AZD6244 in Combination With Docetaxel Versus Docetaxel Alone in KRAS Mutation Positive Non Small Cell Lung Cancer (NSCLC) Patients
ClinicalTrials.gov NCT00888134 AZD6244 in Cancers With BRAF Mutations

more info…………………………………….

AZD-6244 (Selumetinib) is an orally-available, aminobenzimidazole-based, allosteric inhibitor of MEK1 kinase with an IC50 of 14 nM. [1] IC50 concentrations of
In cellular growth assays, AZD-6244 was more potent in cell lines containing activating B-Raf and Ras mutations, with IC50 values ranging from 59 to 473 nM. In HT-29 and Malme-3M cell studies, AZD-6244 was found to induce G1-S cell cycle arrest, inducing apoptosis after a 2-day incubation period. [1] In Colo-205 xenografts, AZD6244 induced increased levels of cleaved caspase-3, indicating apoptosis. [2]

In diffuse large B-cell lymphoma (DLBCL) lines, nanomolar concentration of AZD-6244 effectively downregulated MEK/ERK target substrates, including c-Myc, Mcl-1, and Bcl-2. [3]

Technical information:

Chemical Formula:		C₁₇H₁₅BrClFN₄O₃
CAS #:		606143-52-6
Molecular Weight:		457.68

Appearance:		White
Chemical Name:		6-(4-bromo-2-chlorophenylamino)-7-fluoro-N-(2-hydroxyethoxy)-3-methyl-3H-benzo[d]imidazole-5-carboxamide
Solubility:		Up to 100 mM in DMSO
Synonyms:		AZD-6244, AZD 6244, AZD6244, Selumetinib, Selumetinib sulfate, NSC-748727, ARRY-142886

Reference:

1.	Yeh et al., Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin. Cancer Res. 2007, 13, 1576-1583 Pubmed ID: 17332304
2.	Davies et al., AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models. Mol. Cancer Ther. 2007, 6, 2209-2219. Pubmed ID: 17699718
3.	Bhalla et al., The novel anti-MEK small molecule AZD6244 induces BIM-dependent and AKT-independent apoptosis in diffuse large B-cell lymphoma. Blood, 2011, 118(4), 1052-1061. Pubmed ID: 21628402

Diabetes – LX4211

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Jul 222013

A compound is being investigated as a Type II diabetes treatment by Lexicon Pharmaceuticals, although it is in an early stage of development

LX4211

A compound is being investigated as a Type II diabetes treatment by Lexicon Pharmaceuticals, although it is in an early stage of development.

LX4211 is not selective for just sodium glucose co-transporter-2, or SGLT-2 – it also inhibits SGLT-1.1 Inhibiting this second transporter, responsible for the absorption of glucose in the intestines, it also results in an increase in the release of glucagon-like peptide-1 (GLP-1), but might be combated by administering the dual inhibitor in combination with a dipeptidyl peptidase-4 (DPP-4) inhibitor to prevent it being activated.

– See more at:

http://www.manufacturingchemist.com/technical/article_page/Diabetes__LX4211/88179

http://www.manufacturingchemist.com/technical/article_page/Diabetes__LX4211/88179#sthash.BVOa03IT.dpuf