A new peptidomimetic inhibits prostate cancer’s growth by
preventing the androgen receptor from binding to its cofactorRead more
http://www.chemistryviews.org/details/news/4884471/Preventing_Dangerous_Liaisons.html
Showing posts with label medicinal chemistry. Show all posts
Showing posts with label medicinal chemistry. Show all posts
Monday 24 June 2013
Preventing Dangerous Liaisons
A new peptidomimetic inhibits prostate cancer’s growth by
preventing the androgen receptor from binding to its cofactorRead more
http://www.chemistryviews.org/details/news/4884471/Preventing_Dangerous_Liaisons.html
Gut Feeling for Obesity Treatment
Gut Feeling for
Obesity Treatment
Newly synthesized benzimidazole-type compounds work directly
in the gut rather than circulating in the blood to lower triglyceridesRead more
http://www.chemistryviews.org/details/news/4907951/Gut_Feeling_for_Obesity_Treatment.html
Sunday 23 June 2013
Silibinin (INN), also known as silybin, is the major active constituent of silymarin, a standardized extract of the milk thistle seeds containing mixture of flavonolignans consisting of among others of silibinin, isosilibinin, silicristin, and silidianin
Silibinin (INN), also known as silybin, is the major active constituent of silymarin, a standardized extract of the milk thistle seeds containing mixture of flavonolignans consisting of among others of silibinin, isosilibinin, silicristin, and silidianin. Silibinin itself is mixture of two diastereomers silibinin A and silybinin B in approximately equimolar ratio. Both in vitro and animal research suggest that silibinin has hepatoprotective (antihepatotoxic) properties that protect liver cells against toxins.[1][2] Silibinin has also demonstrated in vitro anti-cancer effects against human prostate adenocarcinoma cells, estrogen-dependent and -independent human breast carcinoma cells, human ectocervical carcinoma cells, human colon cancer cells, and both small and nonsmall human lung carcinoma cells.[3][4][5][6]
Chemically modified silibinin, silibinin dihydrogen disuccinate disodium (trade name Legalon SIL) a solution for injection, is currently being tested as a treatment of severe intoxications with hepatotoxic substances, such as death cap (Amanita phalloides) poisoning.[7] There is also clinical evidence for the use of silibinin as a supportive element in alcoholic and Child grade ‘A’ liver cirrhosis.[8]
FROM SILYBUM MARIANUM (L.) GAERTN.
A NEW NATURAL PREVENTIVE TARGETED AT THE LIVER
The liver, due to the vital role it plays in metabolism, is particularly exposed to the harmful action of endogenous and exogenous toxic substances. In fact, many potentially harmful molecules (alcohol, drugs, hormones, etc.) are metabolized by the liver and transformed into more hydro-soluble derivatives for subsequent biliary extraction and removal from the body. This detoxication process is achieved by a variety of enzymes (oxidizing, reducing, hydrolyzing or conjugating) located in the hepatic microsomes, part of the smooth endoplasmic reticulum of the liver cell. For this reason the upkeep of the integrity of the liver cell is necessary for the safeguarding of health. Several biochemical reactions involve as starters or intermediates various free radical species which constitute a continuous risk factor for the integrity of the hepatocytes.Therefore, any prevention aimed at reducing potential damage to the liver and any substances contributing to its integrity are certainly of interest. Derivatives of the traditionally used European plant Silybum marianum (L.) Gaertn. (Asteraceae) occupy an eminent position in liver protection. The name Silybum derives from "sillybon" (tuft, pendant), an ancient Greek word used by Dioscorides (I century A.D.) to indicate a thistle with white spotted leaves. An old legend tells that these white marks and stripes on the leaves represent the drops of Mary's milk fallen from her breast while she was breastfeeding Jesus during their escape to Egypt.2 Since ancient times
S. marianum
has been known and used to be recommended as an emetic. During the
Middle Ages the plant was probably cultivated in monasteries and used
for medicinal purposes: the roots, herb and leaves were recommended for
swelling and erysipelas (St. Hildegard from Bingen, 1098-1179) or for
the treatment of liver complaints (Lonicerus, John Gerard, Pietro Andrea
Mattioli, XVI-XVII centuries). From 1755 onwards, the specific use of
S. marianum fruit for the treatment of liver disease, disorders of the bile duct and spleen was documented. At present, the standardized extract (silymarin) obtained from the fruit of
S. marianum and containing as main constituents silybin,
silydianin and silychristin (Fig.1), is widely used in European medicine
in the treatment of liver disease. The main constituent silybin has
been subjected to several biochemical and pharmacological studies which
have demonstrated its interesting properties but also its poor
bioavailability. Complexation with soy phosphatidylcholine gives rise to
the lipophilic complex (US Patent 4, 764, 508) which
substantially improves the bioavailibility of silybin. This results in a
marked preventive action as observed in several models of liver
intoxication including those with a strong involvement of oxidative
stress. In this way, the silybin-phosphatidylcholine complex
SILIPHOS®, containing 33% of silybin, endowed with antioxidant activity
and, simultaneously, able to prevent cellular derangement by
stabilizing the cell membranes and restoring the normal ultrastructure
of the hepatocytes, plays a key role in the prevention of liver damage.http://www.swansonvitamins.com/health-library/products/siliphos.html- Al-Anati L, Essid E, Reinehr R, Petzinger E (2009). "Silibinin protects OTA-mediated TNF-alpha release from perfused rat livers and isolated rat Kupffer cells". Molecular Nutrition & Food Research 53 (4): 460–6. doi:10.1002/mnfr.200800110. PMID 19156713.
- Jayaraj R, Deb U, Bhaskar AS, Prasad GB, Rao PV (2007). "Hepatoprotective efficacy of certain flavonoids against microcystin induced toxicity in mice". Environmental Toxicology 22 (5): 472–9. doi:10.1002/tox.20283. PMID 17696131.
- Mokhtari MJ, Motamed N, Shokrgozar MA (2008). "Evaluation of silibinin on the viability, migration and adhesion of the human prostate adenocarcinoma (PC-3) cell line". Cell Biology International 32 (8): 888–92. doi:10.1016/j.cellbi.2008.03.019. PMID 18538589.
- Bhatia N, Zhao J, Wolf DM, Agarwal R (1999). "Inhibition of human carcinoma cell growth and DNA synthesis by silibinin, an active constituent of milk thistle: comparison with silymarin". Cancer Letters 147 (1–2): 77–84. doi:10.1016/S0304-3835(99)00276-1. PMID 10660092.
- Hogan FS, Krishnegowda NK, Mikhailova M, Kahlenberg MS (2007). "Flavonoid, silibinin, inhibits proliferation and promotes cell-cycle arrest of human colon cancer". Journal of Surgical Research 143 (1): 58–65. doi:10.1016/j.jss.2007.03.080. PMID 17950073.
- Sharma G, Singh RP, Chan DC, Agarwal R (2003). "Silibinin induces growth inhibition and apoptotic cell death in human lung carcinoma cells". Anticancer Research 23 (3B): 2649–55. PMID 12894553.
- Mitchell, T (2009). "Intravenous Milk thistle (silibinin-legalon) for hepatic failure induced by amatoxin/Amanita mushroom poisoning". (Clinical study).
- Saller R, Brignoli R, Melzer J, Meier R (2008). "An updated systematic review with meta-analysis for the clinical evidence of silymarin". Forschende Komplementärmedizin (2006) 15 (1): 9–20. doi:10.1159/000113648. PMID 18334810. Retrieved 2010-12-14.
Saturday 22 June 2013
Friday 21 June 2013
.Artificial sweetener a potential treatment for Parkinson’s disease.
Mannitol, a sugar alcohol produced by fungi, bacteria,
and algae, is a common component of sugar-free gum and candy. The sweetener is
also used in the medical field — it’s approved by the FDA as a diuretic to flush
out excess fluids and used during surgery as a substance that opens the
blood/brain barrier to ease the passage of other drugs.
Now Profs. Ehud Gazit and Daniel Segal of Tel Aviv University‘s Department of Molecular Microbiology
and Biotechnology and the Sagol School of Neuroscience, along with their
colleague Dr. Ronit Shaltiel-Karyo and PhD candidate Moran Frenkel-Pinter, have
found that mannitol also prevents clumps of the protein α-synuclein from forming
in the brain — a process that is characteristic of Parkinson’s disease.Read more at
Thursday 20 June 2013
Ambrx partners with Zhejiang for breast cancer antibody drug conjugate development
|
http://contractresearch.pharmaceutical-business-review.com/news/ambrx-partners-with-zhejiang-for-breast-cancer-antibody-drug-conjugate-development-170613
Tuesday 18 June 2013
Monday 17 June 2013
Incyte Drug Jakafi ® (ruxolitinib) Improved Overall Survival in Phase III Trial of Patients with Myelofibrosis
ruxolitinib
Incyte Drug Jakafi®ruxolitinib Improved Overall Survival in Phase III Trial of Patients with Myel. by Business Wirevia The Motley Fool Jun 16th 2013 220AM ... The phase III Controlled Myelofibrosis Study with Oral JAK Inhibitor-I (COMFORT-I) and COMFORT-II trials showed significant benefits by reducing spleen size, relieving debilitating symptoms, and improving overall survival  |
ABILIFY® Granted Additional Approval as Adjunctive Therapy for the Treatment of Depression in Japan
http://japan.pharmaintellect.com/2013/06/abilify-granted-additional-approval-as.html?utm_source=feedburner&utm_medium=email&utm_campaign=Feed%3A+Pharmainvest+%28PharmaInvest%29
Ibrutinib Phase 2 Data: Analyses Show Efficacy with Ibrutinib Monotherapy in Patients with Relapsed or Refractory Mantle Cell or Diffuse Large B-cell Lymphoma
ibrutinib
June 16, 2013
Janssen Research & Development, LLC (Janssen), today announced the results of two separate Phase 2 studies suggesting that ibrutinib, an investigational oral Bruton's tyrosine kinase (BTK) inhibitor, shows efficacy when used as a monotherapy in patients with relapsed/refractory mantle cell lymphoma (MCL) or diffuse large B-cell lymphoma (DLBCL). The studies were presented today at the European Hematology Association (EHA) 18th Annual Congress in Stockholm, Sweden. Ibrutinib is being jointly developed by Janssen and Pharmacyclics, Inc.
Ibrutinib (USAN), also known as PCI-32765, is an experimental drug candidate for the treatment of various types of cancer. It is an orally-administered, selective and covalent inhibitor of the enzyme Bruton tyrosine kinase (Btk).
Ibrutinib is currently under development by Pharmacyclics, Inc and Johnson & Johnson's Janssen Pharmaceutical division for B-cell malignancies including chronic lymphocytic leukemia, mantle cell lymphoma, diffuse large B-cell lymphoma, and multiple myeloma.
Ibrutinib was first designed and synthesized at Celera Genomics by Zhengying Pan, who along with a team of chemists and biologists reported in 2007 a structure-based approach for creating a series of small molecules that inactivate BTK through covalent binding to cysteine-481 near the ATP binding domain of BTK[2].
These small molecules irreversibly inhibited BTK by using a Michael acceptor for binding to the target cysteine.
In April 2006, Pharmacyclics acquired Celera’s small molecule BTK inhibitor discovery program, which included a compound, PCI-32765 (known as compound 13 in the Pan et al paper) that was subsequently chosen for further preclinical development based on the discovery of anti-lymphoma properties in vivo .
Since 2006, Pharmacyclics’ scientists have advanced the molecule into clinical trials and identified specific clinical indications for the drug. It also has potential effects against autoimmune arthritis.
Sunday 16 June 2013
Pharma-Execs-2012-Pipeline-Report
Just days before this article went to press, FDA approved the first of a new kind of oral enzyme treatment that mediates cellular response, Incyte/Novartis' Jakafi, for a rare bone marrow disease called myelofibrosis. The next JAK inhibitor, Pfizer's toficitinib, could hit the market late next year, meaning a lot of rheumatoid arthritis patients will never again have to sit in a hospital for a couple of hours to get an anti-TNF infusion. Many innovative drugs, long out of the gate, are closing in on the finish line; science is back, and a better understanding of the way genomics shapes disease is bringing about better outcomes, and sometimes faster approvals.
read all at
http://www.pharmexec.com/pharmexec/Deals/Pharm-Execs-2012-Pipeline-Report/ArticleStandard/Article/detail/752361?contextCategoryId=48159
Thursday 13 June 2013
AstraZeneca buys Pearl Therapeutics in $1.15bn deal
AstraZeneca buys Pearl Therapeutics in $1.15bn deal
The UK's second largest drug company, AstraZeneca, has announced that it will buy US based lung disease drug specialist, Pearl Therapeutics, in a deal worth up to $1.15bn (£742m).
http://www.pharmaceutical-technology.com/news/newsastrazeneca-buys-pearl-therapeutics-in-115bn-deal?WT.mc_id=DN_News
PFIZER, MERCK, SANOFI --Does This Pipeline Promise Tomorrow's Blockbuster Sales?
Does This Pipeline Promise Tomorrow's Blockbuster Sales?
Motley Fool
Pfizer's future looks strong with its robust pipeline that boasts 74 total drugs in development, and at least in late-stage candidates, Merck looks strong as well, with another 23 therapies in phase 2 development. However, it's the quality, not the ...
read all at
http://www.fool.com/investing/general/2013/06/12/does-this-pipeline-promise-tomorrows-blockbuster-s.aspx
Wednesday 12 June 2013
Roche's RoActemra gets EU OK for rare child arthritis
The European Medicines Agency has expanded approval for Roche's RoActemra to cover the treatment of children with polyarticular juvenile idiopathic arthritis.
The regulator has decreed that RoActemra (tocilizumab) can be used to treat patients two years of age and older who have not responded adequately to treatment with methotrexate. The drug can be given alone or in combination with MTX.
Tocilizumab(INN, or atlizumab, developed by Hoffmann–La Roche and Chugai and sold under the trade names Actemra and RoActemra) is an immunosuppressive drug, mainly for the treatment of rheumatoid arthritis (RA) and systemic juvenile idiopathic arthritis, a severe form of RA in children. It is a humanized monoclonal antibody against the interleukin-6 receptor (IL-6R). Interleukin 6 (IL-6) is a cytokine that plays an important role in immune response and is implicated in the pathogenesis of many diseases, such asautoimmune diseases, multiple myeloma and prostate cancer.
Will nanorods be the next big male contraceptive idea?
| |
Successful experiments on mice bode well for a future human contraceptive - if men can stomach the injections
Pet contraception is considered an important topic, given the four million unwanted dogs and cats that are thought to be put down every year in the US alone. Many vets routinely sterilise pets, but since surgery requires time and expertise scientists have been looking for cheaper, simpler alternatives. | |
Functionalising the nanorods with methoxy poly(ethylene glycol) enables them to be used for contraception or even sterilisation © ACS
New Fluzone Quadrivalent Four-Strain Influenza Vaccine from Sanofi Pasteur Now Licensed By FDA for Broad Age Range of Children and Adults
http://www.drugs.com/newdrugs/new-fluzone-quadrivalent-four-strain-influenza-vaccine-sanofi-pasteur-now-licensed-fda-broad-age-3810.html
Influenza (Flu)
90Y-Epratuzumab Study Shows Improvement of Therapy Results Following R-CHOP
June 10, 2013 (GLOBE NEWSWIRE) -- Immunomedics, Inc. (Nasdaq:IMMU), a biopharmaceutical company primarily focused on the development of monoclonal antibody-based products for the targeted treatment of cancer, autoimmune and other serious diseases, today reported that adding two doses of epratuzumab labeled with the radioisotope, yttrium-90 (90Y), to a combination of rituximab and CHOP chemotherapy (R-CHOP), the standard of care for patients with diffuse large B-cell lymphoma (DLBCL), appeared to improve elderly patients' responses to treatment.
read all at
http://www.drugs.com/clinical_trials/90y-epratuzumab-study-shows-improvement-therapy-results-following-r-chop-15714.html
by
WORLD DRUG TRACKER
DR ANTHONY
Tuesday 11 June 2013
Infinity Pharmaceuticals And IPI-145: ASCO 2013 Highlights
Infinity Pharmaceuticals And IPI-145: ASCO 2013 Highlights
Seeking Alpha
In June 2012, Infinity suffered a significant writedown when its cancer drug, saridegib proved ineffective in a Phase II clinical trial. The company restructured financing deals with Takeda Pharmaceutical Company, Purdue Pharmaceutical Products, and ...
http://seekingalpha.com/article/1491062-infinity-pharmaceuticals-and-ipi-145-asco-2013-highlights?source=google_news
 |
BY WORLD DRUG TRACKER
Blocking Biosimilars
Blocking Biosimilars
As the U.S. Food and Drug Administration (FDA) continues to finalize regulations
to establish a pathway for approving biopharmaceutical or biosimilar drugs,
leading branded drug manufacturers are looking ahead and lobbying state
legislatures to enact laws that would limit the substitution of biogenerics for
brand-name drugs. Currently, pharmacists in most states can substitute
lower-cost generics for branded chemical or small-molecule drugs without such
approval.
BY WORLD DRUG TRACKER
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