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Tag Archives: CANCER
Dulaglutide Shows Superiority in Phase 3 Trials

DULAGLUTIDE
STRUCTURAL FORMULA
Monomer
HGEGTFTSDV SSYLEEQAAK EFIAWLVKGG GGGGGSGGGG SGGGGSAESK 50
YGPPCPPCPA PEAAGGPSVF LFPPKPKDTL MISRTPEVTC VVVDVSQEDP 100
EVQFNWYVDG VEVHNAKTKP REEQFNSTYR VVSVLTVLHQ DWLNGKEYKC 150
KVSNKGLPSS IEKTISKAKG QPREPQVYTL PPSQEEMTKN QVSLTCLVKG 200
FYPSDIAVEW ESNGQPENNY KTTPPVLDSD GSFFLYSRLT VDKSRWQEGN 250
VFSCSVMHEA LHNHYTQKSL SLSLG 275
Disulfide bridges location
55-55′ 58-58′ 90-150 90′-150′ 196-254 196′-254′
http://www.ama-assn.org/resources/doc/usan/dulaglutide.pdf
7-37-Glucagon-like peptide I [8-glycine,22-glutamic acid,36-glycine] (synthetic
human) fusion protein with peptide (synthetic 16-amino acid linker) fusion protein with
immunoglobulin G4 (synthetic human Fc fragment), dimer
Eli Lilly and Co. announced detailed safety and efficacy results from three Phase 3 AWARD trials for dulaglutide, an investigational, long-acting glucagon-like peptide 1 (GLP-1) receptor agonist being studied as a once-weekly treatment for type 2 diabetes
Sponge molecules isolated and synthesized for drug trials
By scouring the oceans for disease-fighting molecules, researchers have identified two new anticancer compounds. Isolated from a sea sponge, the compounds represent a new class of the natural products called polyketides, many of which have biological activity. Because it’s not possible to extract sufficient amounts of the molecules from the sponges, the researchers also devised chemical syntheses that allowed them to make enough material to initiate clinical trials on one of the substances,
Cancer Fighters From The Sea
Natural Products: Sponge molecules isolated and synthesized for drug trials.
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Let’s Set a Global Drug Quality Benchmark by Kiran M Shaw, Biocon

With Indian-made generics accounting for a US market share of over 25 per cent, it is not surprising that it is gaining significant mindshare of the Food and Drug Administration ( FDA). The spate of quality issues with leading Indian pharmaceutical companies in the past couple of years however should not be viewed in isolation. Big Pharma in the West, too, has been facing increasing flak from the FDA and other regulators over good manufacturing practice ( GMP) violations. High profile names like J& J, Genzyme (Sanofi), GSK, Sandoz, Watson, Teva and many others have encountered their share of quality problems and have been served with ‘warning letters’ from FDA
http://kiranmazumdarshaw.blogspot.in/2013/06/lets-set-global-drug-quality-benchmark.html
READ ALL AT THE LINK ABOVE
Study Finds Substances from African Medicinal Plants Could Help Stop Tumour Growth

Sections of the root of the giant globe thistle.
photo: Victor Kuete, Institute of Pharmaceutical Sciences and Biochemistry
African medicinal plants contain chemicals that may be able to stop the spread of cancer cells. This is the conclusion of researchers following laboratory experiments conducted at Johannes Gutenberg University Mainz (JGU). The plant materials will now undergo further analysis in order to evaluate their therapeutic potential.
“The active substances present in African medicinal plants may be capable of killing off tumour cells that are resistant to more than one drug. They thus represent an excellent starting point for the development of new therapeutic treatments for cancers that do not respond to conventional chemotherapy regimens,” explained Professor Thomas Efferth of the Institute of Pharmaceutical Sciences and Biochemistry – Therapeutic Life Sciences at Mainz University. For the past four years, Efferth and biochemist Dr. Victor Keute of the University of Dschang in Cameroon have been studying the active substances in African plants such as the giant globe thistle, wild pepper, speargrass, and Ethiopian pepper.
Tesaro and the European Network of Gynecological Oncological Trial Groups Forge Partnership to Develop Niraparib for Ovarian Cancer

Niraparib; MK 4827
MOLECULAR FORMULA C19H20N4O
MOLECULAR WEIGHT 320.4
SPONSOR Merck Sharp & Dohme Corp.
CAS REGISTRY NUMBER 1038915-60-4
THERAPEUTIC CLAIM Antineoplastic
CHEMICAL NAMES
1. 2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]-
2. 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide
TESARO and the European Network of Gynecological Oncological Trial Groups (ENGOT) Forge Partnership to Develop Niraparib for Ovarian Cancer
June 3, 2013 — TESARO, Inc. an oncology-focused biopharmaceutical company, and the European Network of Gynecological Oncological Trial Groups (ENGOT), a network of national and regional clinical trial organizations, today announced a partnership for the Phase 3 clinical development of niraparib, an orally active, potent poly (ADP-ribose) polymerase (PARP) inhibitor. READ ALL AT http://www.pharmalive.com/tesaro-and-the-european-network-of-gynecological-oncological-trial-groups-forge-partnership-to
http://www.ama-assn.org/resources/doc/usan/niraparib.pdf
http://clinicaltrials.gov/show/NCT01847274
MK-4827:
MK-4827 is a potent, Selective, PARP 1/2 inhibitor with IC50 of 3.8 and 2.1 nM for PARP1 and 2, respectively. MK-4827 possesses potential Antineoplastic Activity. In a Whole Cell assay, MK -4827 prevented PARP activity with an EC50 of 4 nM, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. MK-4827 induces selective synthetic lethality in homologous recombination (HR) repair deficient tumors with BRCA1 / 2 loss and tumor cell lines with non-BRCA-related HR defects, supporting clinical utility in sporadic tumors. MK-4827 reveals good pharmacokinetic properties and is currently in phase I clin. trials. The phase I clinical trials for MK-4827 is ongoing in the treatment of solid tumors.
BY WORLD DRUG TRACKER
New Drug Ganetespib May Help Fight Certain Advanced Lung Cancers

ganetespib
STA 9090, cas no 888216-25-9
read all at
http://www.drugs.com/news/new-may-help-fight-certain-advanced-lung-cancers-44819.html
by
WORLD DRUG TRACKER
DR ANTHONY CRATO
Top 10 experimental cancer drugs – 2013
Top 10 experimental cancer drugs – 2013
New Drug May Help Immune System Fight Cancer
read all at
http://www.drugs.com/news/new-may-help-immune-fight-cancer-44582.html
Turning Off Cancer’s “Master Regulator”
Researchers have identified a gene that, when repressed in tumor cells, puts a halt to cell growth and a range of processes needed for tumors to enlarge and spread to distant sites. The Johns Hopkins researchers hope that this “master regulator” gene may be the key to developing a new treatment for tumors resistant to current drugs………from……………..
GENNewsHighlights
read all at
http://www.genengnews.com/gen-news-highlights/turning-off-cancer-s-master-regulator/81248318/
US HERBS- FIGHT CANCER WITH BROCCOLI
An example of the superfoods is the broccoli. Broccoli belongs to the cruciferous group of vegetables. Naturally, broccoli is an an excellent source of vitamins, minerals and fiber. These are elements from Nature that have been extensively studied.
Epidemiological studies provideevidence that the consumption of this vegetable protects against cancer. The protection against cancer is mainly derived from altering estrogen metabolism and antioxidant properties, enhancing detoxification, decreasing carcinogen coumpound activation, slowing tumor growth and inducing cancer cell apoptosis (death). Such attributes qualify broccoli as a superfood.
American Institute of Cancer Research estimates that a daily intake of three servings would potentially reduce cancer rates by 20%.
Broccoli contains certain chemicals that may reduce the risk of colorectal or other cancers, although it is not clear which individual compounds may be responsible for the protective effects. While research in this area continues, the best advice at this time to reduce cancer risk is to eat a wide variety of vegetables. It is reasonable to include broccoli as part of a balanced diet.
roccoli has been around for more than 2,000 years but has only been commercially grown in the United States since the 1920s. Today, more than 90% of the broccoli harvested in the United States comes from California, although it is also grown in other parts of the country.
About 2 decades ago, researchers first suggested a possible link between diets high in cruciferous vegetables (a group of plants including cauliflower, cabbage, broccoli, and Brussels sprouts)) and a lower risk of cancer. However, it was not until the 1990s that certain chemicals found in broccoli were identified as possible cancer-preventing compounds. In 1997, a study was published that noted broccoli sprouts had higher levels of one of these compounds than mature broccoli.
Broccoli is a plant in the cabbage family, whose large flower head is used as a vegetable. The word broccoli, from the Italian plural of broccolo, refers to “the flowering top of a cabbage”. Broccoli is usually boiled or steamed but may be eaten raw and has become popular as a raw vegetable in hors d’œuvre trays. The leaves may also be eaten.
Broccoli is classified in the Italica cultivar group of the species Brassica oleracea. Broccoli has large flower heads, usually green in color, arranged in a tree-like structure on branchessprouting from a thick, edible stalk. The mass of flower heads is surrounded by leaves. Broccoli most closely resembles cauliflower, which is a different cultivar group of the same species.
Broccoli was derived from cultivated leafy cole crops in the Northern Mediterranean in about the 6th century BCE. Since the Roman Empire, broccoli has been considered a uniquely valuable food among Italians. Broccoli was brought to England from Antwerp in the mid-18th century by Peter Scheemakers. Broccoli was first introduced to the United States by Italian immigrants but did not become widely known there until the 1920s
Broccoli is high in vitamin C and dietary fiber; it also contains multiple nutrients with potent anti-cancer properties, such as diindolylmethane and small amounts of selenium. A single serving provides more than 30 mg of vitamin C and a half-cup provides 52 mg of vitamin C. The 3,3′-Diindolylmethane found in broccoli is a potent modulator of theinnate immune response system with anti-viral, anti-bacterial and anti-cancer activity. Broccoli also contains the compound glucoraphanin, which can be processed into an anti-cancer compound sulforaphane, though the benefits of broccoli are greatly reduced if the vegetable is boiled. Broccoli is also an excellent source of indole-3-carbinol, a chemical which boosts DNA repair in cells and appears to block the growth of cancer cells.
Boiling broccoli reduces the levels of suspected anti-carcinogenic compounds, such as sulforaphane, with losses of 20–30% after five minutes, 40–50% after ten minutes, and 77% after thirty minutes. However, other preparation methods such as steaming,microwaving, and stir frying had no significant effect on the compounds.
Broccoli has the highest levels of carotenoids in the brassica family.[17] It is particularly rich in lutein and also provides a modest amount of beta-carotene.
A high intake of broccoli has been found to reduce the risk of aggressive prostate cancer. Broccoli consumption may also help prevent heart disease.
Broccoli sprouts are often suggested for their health benefits
| Nutritional value per 100 g (3.5 oz) | |
|---|---|
| Energy | 141 kJ (34 kcal) |
| Carbohydrates | 6.64 g |
| – Sugars | 1.7 g |
| – Dietary fiber | 2.6 g |
| Fat | 0.37 g |
| Protein | 2.82 g |
| Water | 89.3 g |
| Vitamin A equiv. | 31 μg (4%) |
| – beta-carotene | 361 μg (3%) |
| – lutein and zeaxanthin | 1403 μg |
| Thiamine (vit. B1) | 0.071 mg (6%) |
| Riboflavin (vit. B2) | 0.117 mg (10%) |
| Niacin (vit. B3) | 0.639 mg (4%) |
| Pantothenic acid (B5) | 0.573 mg (11%) |
| Vitamin B6 | 0.175 mg (13%) |
| Folate (vit. B9) | 63 μg (16%) |
| Vitamin C | 89.2 mg (107%) |
| Vitamin E | 0.78 mg (5%) |
| Vitamin K | 101.6 μg (97%) |
| Calcium | 47 mg (5%) |
| Iron | 0.73 mg (6%) |
| Magnesium | 21 mg (6%) |
| Manganese | 0.21 mg (10%) |
| Phosphorus | 66 mg (9%) |
| Potassium | 316 mg (7%) |
| Zinc | 0.41 mg (4%) |
| Link to USDA Database entry Percentages are relative to US recommendations for adults. Source: USDA Nutrient Database
Broccoli is considered a good source of nutrients because it is rich in vitamin C, carotenoids (vitamin A-like substances), fiber, calcium, and folate. Broccoli is also a source of many substances called phytochemicals, or plant chemicals, that may have anticancer properties. For example, broccoli contains several compounds called isothiocyanates, including sulforaphane and indole-3-carbinol (I3C), which have been touted as possible anti-cancer agents in recent years. Early studies have shown these substances may act as anti-oxidants and may boost detoxifying enzymes in the body. Some studies have also suggested they may alter the levels of estrogen in the body, which might affect breast cancer risk.The chemical composition of broccoli and other cruciferous vegetables is complex, which makes it hard to determine which compound or combination of compounds may provide protection against cancer. Eating a wide variety of plant-based foods may be the best way to get the necessary components.Some researchers suggest that small amounts of broccoli sprouts may protect against the risk of cancer as effectively as much larger amounts of the mature vegetable. We are not aware of any clinical studies that have been done in humans to verify this claim.Another substance in broccoli, indole-3-carbinol (I3C), seems to alter estrogen levels and may also raise levels of protective enzymes in the body. Several studies of cancer cells growing in laboratory dishes or flasks have shown it may slow or stop the growth of breast, prostate, and other cancer cells. Some early studies in animals have shown similar results. Small studies in humans have found it may prevent the development of pre-cancerous growths in the cervix, as well as growths called papillomas in the throat. Again, larger studies are needed to find out what benefits I3C may have against cancer. THE MOLECULES The active molecules are Indole-3-carbinol (1H-indol-3-ylmethanol IUPAC name) OR I3C and isothiocyanates (mostly sulforaphane: 1-Isothiocyanato-4-methylsulfinylbutane). Indole-3-carbinol has a indole with a hydroxymethyl group that represents the hydrophilic group. Sulfurofane is a isothiocyanate, it means that it has a –N=C=S chemical group, formed by substituting sulfur for oxygen in the isocyanate group, bounded to a big alkyl chain containing a sulfinyl S=O group. Both indole-3-carbinol and sulphoraphane derive from glucosinolates. Glucosinolates are a class of organic compounds that contain sulfur and nitrogen and are derived from glucose and an amino acid. They occur as secondary metabolites of almost all plants of the order Brassicales. GENERAL EFFECTS ON HEALTH I3C has been shown to have a chemopreventive action on several human cancers. The first and greatest effects concern breast and cervical estrogen-dependant cancer. Later, many researches managed to relate I3C with the prevention from colon, lung and prostate cancer too. The micronutrient indole-3-carbinol: implications for disease and chemoprevention, 2000 Sulforaphane, like I3C, is useful against many types of cancer. Moreover, it has antimicrobial properties, as it appears to help eradicate Helicobacter Pylori from the stomach. Molecular targets of dietary phenethyl isothiocyanate and sulforaphane for cancer |
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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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