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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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AYURVEDA HERBS-HOLY BASIL (Ocimum sanctum)
HOLY BASIL (Ocimum sanctum): Also known as Tulsi, this plant is actually considered sacred by many people in India. As such, it can be found growing in temple gardens, where the rich fragrance opens respiratory passages and some say, help the spirit soar.
Tulsi is one of the most sacred plants of India. Basil opens the heart and mind, bestowing the energy of love and devotion. Basil strengthens the immune system, increasing prana or life force and improving the memory. A nerve tonic, improving absorption and strengthening the nerve tissue, also used externally for various skin conditions. This plant is found in most East Indian households as it absorbs positive ions, energizes negative ions, and liberates ozone from the suns rays. Found in our spicenlightenment Vata aromatherapy Candle and spicebodhi Vata body bar.
Holy Basil’s key compounds, including eugenol and caryophyllene, are similar to those found in oregano (Origanum vulgare) and it shares the anti-inflammatory, antipyretic, and analgesic actions typical of the oregano family (Padalia RC, Verma RS. Nat Prod Res. 2011;25(6):569-75. Godhwani S, et al. J Ethnopharmacol. 1987;21:153-63).
This plant is also native to West Africa. In Sierra Leone, it is called ‘Fever Plant.’ The various fixed oil compounds found in the plant have shown extensive antimicrobial and antifungal activity against a variety of pathogens including Escherichia coli and Candida albicans. In classical Ayurveda, Holy Basil was used as an anti-tussive, to clear “excess dampness in the lungs.” Recent human trials have validated this, the data showing that this herb can increase lung capacity as well as reduce labored breathing.
It has also been shown to significantly reduce several measures of stress in generalized anxiety disorder (GAD) patients.
Holy basil can be taken in capsule, tea and in liquid forms. It is dispensed in 600-700 mg doses, twice daily, before meals. Allow 2-4 weeks for optimal results.
Ayurveda- Turmeric, Antiarthritic properties
Turmeric (Curcuma longa) is a rhizomatous herbaceous perennial plant of the ginger family, Zingiberaceae. It is native to tropical South Asia and needs temperatures between 20°C and 30°C (68°F and 86°F) and a considerable amount of annual rainfall to thrive. Plants are gathered annually for their rhizomes, and propagated from some of those rhizomes in the following season. In Vietnam, turmeric is called “nghệ”, “củ nghệ”.
When not used fresh, the rhizomes are boiled for several hours and then dried in hot ovens, after which they are ground into a deep orange-yellow powder commonly used as a spice in curries and other South Asian and Middle Eastern cuisine, for dyeing, and to impart color to mustard condiments. Its active ingredient is curcumin and it has a distinctly earthy, slightly bitter, slightly hot peppery flavor and a mustardy smell
3. Prevented breast cancer from spreading to the lungs in mice.
4. May prevent melanoma and cause existing melanoma cells to commit suicide.
5. Reduces the risk of childhood leukemia.
6. Is a natural liver detoxifier.
7. May prevent and slow the progression of Alzheimer’s disease by removing amyloyd plaque buildup in the brain.
8. May prevent metastases from occurring in many different forms of cancer.
9. It is a potent natural anti-inflammatory that works as well as many anti-inflammatory drugs but without the side effects.
10. Has shown promise in slowing the progression of multiple sclerosis in mice.
11. Is a natural painkiller and cox-2 inhibitor.
12. May aid in fat metabolism and help in weight management.
13. Has long been used in Chinese medicine as a treatment for depression.
14. Because of its anti-inflammatory properties, it is a natural treatment for arthritis and rheumatoid arthritis.
15. Boosts the effects of chemo drug paclitaxel and reduces its side effects.
16. Promising studies are underway on the effects of turmeric on pancreatic cancer.
17. Studies are ongoing in the positive effects of turmeric on multiple myeloma.
18. Has been shown to stop the growth of new blood vessels in tumors.
19. Speeds up wound healing and assists in remodeling of damaged skin.
20. May help in the treatment of psoriasis and other inflammatory skin conditions.
AYURVEDA-SHILAJIT, ANTIAGEING PROPERTIES
A composition comprising Shilajit or an extract thereof in a vitamin and mineral preparation. Shilajit is a compact mass of vegetable organic matter, composed of a gummy matrix interspersed with vegetable fibres and minerals. Substances which have been identified in Shilajit include moisture, gums, albuminoids, calcium, potassium, nitrogen, silica, resin, vegetable matter, magnesium, sulphur, iron, chloride, phosphorous, iodine, glycosides, tannic acid, benzoic acid and a number of vitamins and enzymes.
Shilajit is a natural exudate ejected from rocks during hot weather in the lower Himalayas, Vindhya and other mountain tracts and Nepal, or it may be a tar formed in the earth from the decomposition of vegetable substances. (See the Indian Materia Medica, pages 23 to 32 for a detailed discussion of the composition and properties of Shilajit). It is a compact mass of vegetable organic matter, composed of a gummy matrix interspersed with vegetable fibres and minerals. Shilajit also contains benzoic acid, a compound which, along with its derivatives, has been used as a component of nutritional vitamin and mineral preparations.
Ancient Sanskrit holy texts, over 3,000 years old, make reference to a mysterious substance called shilajit, which they describe as the “destroyer of weakness.” The texts list its powerful health and spiritual benefits and the positive changes that shilajit brought in the lives of those who used it. The sacred substance was prescribed for thousands of years for many different health problems and became a powerful tool in Ayurvedic medicine. There is some indication that shilajit may have been the priceless soma of the Eastern alchemists.
The rediscovery of the power of shilajit is said to have been made by Himalayan villagers observing large white monkeys migrate to the mountains in the warm summer months. The monkeys were seen to be chewing a semi-soft substance that flowed from between layers of rock. The villagers attributed the monkey’s great strength, longevity and wisdom to the strange substance. They began to consume it themselves and reported a broad spectrum of improvements in health. It seemed to give them more energy, relieve digestive problems, Increase sex drive, improve memory and cognition, improve diabetes, reduce allergies, improve the quality and quantity of life and it seemed to cure all diseases.
The ancient Vedic text Rig Veda states that soma “has mountains and stones for its body” and “dwells within the mountainous rock where it grows.” Mountainous rocks are the “abode of soma,” and it is “plucked from between the rocks by mountain dwellers and brought to the priests-alchemists who prepared the soma by washing and grinding and cooking.” Soma was considered the elixir of immortality, the secret substance used by alchemists to perfect both body and mind.
Shilajit must be harvested from sacred cliff sides high in the Himalayan Mountains of Nepal. Millions of years ago, before the Himalayas were formed, a lush garden flourished in a vast fertile valley. The vegetation in that primeval garden became trapped and preserved as the movement of the continents caused that valley to become the tallest mountain range in the world. Today, millions of years later the monsoon rains and extreme freeze and thaw conditions work together to crack large rock formations, exposing the precious shilajit. Because of its ancient nature, the vegetation was never exposed to any type of fertilizer, pesticide, herbicide, or pollution. The native Nepali people collect and carry this gift of nature down the mountain, where it is alchemically processed into a potent, high-quality extract.
This ancient wisdom was passed from generation to generation among the Indian and Nepali alchemists and holy men, but it escaped the notice of the Western medical establishment until the last days of the twentieth century, when explorer John Anderson heard of the amazing benefits of this substance and refused to give up the search until he found its source. He journeyed throughout India and Nepal until he learned of the perilous harvesting the raw shilajit from the cliffs. He also documented the reams of Sanskrit studies showing the rare plant’s benefits. He spoke firsthand with more than fifty Indian and Nepalese researchers that have been studying the wonderful effects of shilajit and perfecting the processes for delivering the purest, most concentrated shilajit ever know to man.
Over sixty years of clinical research have shown that shilajit has positive effects on humans. It increases longevity, improves memory and cognitive ability, reduces allergies and respiratory problems, reduces stress, and relieves digestive troubles. It is anti-inflammatory, antioxidant, and eliminates free radicals. The research proves that shilajit increases immunity, strength, and endurance, and lives up to its ancient reputation as the “destroyer of weakness.”
Technically, shilajit is an exudate that is pressed out from layers of rock in the most sacred and highest mountains in Nepal and other areas. It is composed of humus and organic plant material that has been compressed by layers of rock. Humus is formed when soil microorganisms decompose animal and plant material into elements usable by plants. Plants are the source of all our food and humus is the source of plant food. Unlike other soil humus, shilajit humus consists of 60-80% organic mass.
Shire begins Phase II ‘Vascugel’ trials
April 05,2012
Shire has kicked off two mid-stage trials assessing Vascugel – which is being developed by Shire under the name SRM003 – for enhancing blood vessel repair in patients with end-stage renal disease (ESRD) receiving haemodialysis.
Before patients can undergo haemodialysis, an arteriovenous (AV) access site must be created where blood can be removed, filtered and returned to the body.
In most cases, AV access is achieved through either an AV fistula (AVF), where the vein is connected directly to the artery, or an AV graft, where the vein and artery are connected via a synthetic tube.
Shire notes that there are around 100,000 AV fistulas and 60,000 AV grafts occurring annually in the US. But complications – such as infection, blood clots, and narrowing of the vessel – are common and frequently lead to access failure.
In fact, an estimated 60% of AV grafts fail after one year, requiring an additional procedure to restore flow or to create another access site, Shire said.
AYURVEDA SPOTLIGHT- BRAHMI
Bacopa monnieri
| Bacopa monnieri | |
|---|---|
 |
|
| Scientific classification | |
| Kingdom: | Plantae |
| (unranked): | Angiosperms |
| (unranked): | Eudicots |
| (unranked): | Asterids |
| Order: | Lamiales |
| Family: | Plantaginaceae |
| Genus: | Bacopa |
| Species: | B. monnieri |
Bacopa monnieri (waterhyssop, brahmi, thyme-leafed gratiola, water hyssop) is a perennial, creeping herb whose habitat includes wetlands and muddy shores. Brahmi is also the name given to Centella asiatica, particularly in North India, and Kerala where it is also identified in Malayalam as muttil (മുത്തിള്) or kodakan. This identification of brāhmī as C. asiatica has been in use for long in northern India, as Hēmādri’s Commentary on Aṣṭāṅgahṛdayaṃ (Āyuṛvēdarasāyanaṃ) treats maṇḍūkapaṛṇī (C. asiatica) as a synonym of brahmi, although that may be a case of mistaken identification that was introduced during the 16th century.
Brahmi been used by Indian Ayurvedic medical practitioners for almost 3000 years. The earliest chronicled mention of Brahmi is in several ancient Ayurvedic treatises including the Caraka Samhita (6th century A.D.), in which it is recommended in formulations for the management of a range of mental conditions including anxiety, poor cognition and lack of concentration, and the Bravprakash Var-Prakarana (16th century A.D.).
Description
Bacopa monnieri in Hyderabad, India.
The leaves of this plant are succulent and relatively thick. Leaves are oblanceolate and are arranged oppositely on the stem. The flowers are small and white, with four or five petals. Its ability to grow in water makes it a popular aquarium plant. It can even grow in slightly brackish conditions. Propagation is often achieved through cuttings.
Ecology
It commonly grows in marshy areas throughout India, Nepal, Sri Lanka, China, Taiwan, and Vietnam, and is also found in Florida, Hawaii and other southern states of the USA where it can be grown in damp conditions by the pond or bog garden.
Traditional uses
It has been used in traditional Ayurvedic treatment for epilepsy and asthma. It is also used in Ayurveda for ulcers, tumors, ascities, enlarged spleen, indigestion, inflammations, leprosy, anemia, and biliousness. This plant can be grown even as hydroponics using almost simple water.
Chemical constituents
Bacopa monnieri has many chemical constituents including alkaloids (brahmine and herpestine), saponins (d-mannitol and hersaponin, acid A, and monnierin), flavonoids (luteolin and apigenin). It also contains significant amounts of betulic acid, stigmasterol, beta-sitosterol, and bacopasaponins (bacosides A, bacosides B, bacopaside II, bacopaside I, bacopaside X, bacopasaponin C, bacopaside N2). The minor components include bacopasaponin F, bacopasaponin E, bacopaside N1, bacopaside III, bacopaside IV, and bacopaside V).
Pharmacology of chemical constituents
In rats, bacosides A enhance antioxidant defenses, increasing superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPX) activity.Laboratory studies on rats indicate that extracts of the plant improve memory capacity. Some studies in mice suggest that ingestion of Bacopa for a 12 week period can significantly improve cognitive ability by accelerating the rate of learning and enhanced memory.The sulfhydryl and polyphenol components of Bacopa monnieri extract have also been shown to impact the oxidative stress cascade by scavenging reactive oxygen species, inhibiting lipoxygenase activity and reducing divalent metals.This mechanism of action may explain the effect of Bacopa monniera extract in reducing beta amyloid deposits in a mouse model of Alzheimer’s disease. B. monnieri has a demonstrated ability to reverse diazepam-induced amnesia in the Morris water maze test. The mechanism of this action is unknown. In some trials, bacopacide extract did not restore or enhance memory formation, but improved retention. In others, including a randomized clinical trial of 98 healthy older people (over 55 years), Bacopa significantly improved memory acquisition and retention. A 2012 systematic review found some evidence to suggest that Bacopa improves memory free recall, but there was a lack of evidence for enhancement of other cognitive abilities.
Brahmi may regulate antibody production by augmenting both Th1 and Th2 cytokine production.It may also cause a lower heart rate, and increase secretions in the stomach, intestines, and urinary tract. The increase in secretions may irritate ulcers and urinary tract obstructions.
No safety studies have been performed on brahmi’s use in humans. When a preparation of the plant was evaluated for safety and tolerability it showed no adverse effects but there were some reports of mild gastrointestinal symptoms.
However, participants in a 2001 double-blind study published in Psycho pharmacology experienced side effects including nausea, weakness and dry mouth while taking brahmi, notes the University of Michigan Health System. Brahmi could potentially cause elevated thyroid-hormone levels and decreased sperm counts. Therefore, taking brahmi should be avoided if you have a thyroid condition or are taking thyroid replacement therapies and other medications that affect thyroid function.
Aqueous extract of Bacopa monnieri (Brahmi) has been reported to reversibly suppress spermatogenesis and fertility in male mice with at a dose of 250 mg/kg body weight/day for 28 and 56 days(equivalent to 1.54 g/day for a 76kg male, when properly controlling for animal to human conversions ) Parameters of motility, viability, morphology, and number of spermatozoa in cauda epididymidis returned to baseline 56 days after treatment cessation.
The plant is known by many names in many international languages, including:
- ബ്രഹ്മി in Malayalam
- நீர்ப்பிரமி (Niirpirami)/ Valaarai in Tamil
- ผักมิ (Phak mi), พรมมิ (Phrommi) in Thai
- Lunuwila in Sinhalese (Sri Lanka)
- ae’ ae’ in Hawaiian (Hawaii)
- Rau Đắng in Vietnamese
- פְּשֵטָה שרועה (“psheta sru’a”) in Hebrew\
- conclusions
- Brahmi is a plant that has been used in traditional Indian medicine (Ayurveda). Be careful not to confuse brahmi (Bacopa monnieri) with gotu kola and other natural medicines that are also sometimes called brahmi.Brahmi is used for Alzheimer’s disease, improving memory, anxiety, attention deficit-hyperactivity disorder (ADHD), allergic conditions, irritable bowel syndrome, and as a general tonic to fight stress.People also take brahmi to treat backache, hoarseness, mental illness, epilepsy, joint pain, and sexual performance problems in both men and women. It is also sometimes used as a “water pill.”
-
Brahmi Benefits
Brahmi is considered a nootropic agent, which is the term given to a drug that improves mental functions such as cognition, memory, intelligence, motivation, attention, and concentration. Brahmi has been used in ayurvedic medicine and in traditional treatments for a number of disorders, particularly those involving anxiety, intellect, and poor memory.
Recent major scientific reviews of the plant suggest that it has prominent action on the central nervous system, where it improves understanding, memory, intellect, and speech, and corrects aberrations of emotions, mood, and personality in an individual. Based on the results of human clinical trials, the nootropic effects of Brahmi are thought to manifest after chronic dosing (i.e. 12 weeks) rather than acute (i.e. single day). Studies in humans have shown that chronic administration of Brahmi results in improvements in working memory, visual information processing, learning rate and anxiety.
In India, Brahmi is currently recognized as being effective in the treatment of mental illness and epilepsy. In certain parts of India, Brahmi is believed to be an aphrodisiac; in Sri Lanka, under the name of Loonooweella, Brahmi is prescribed for fevers; in the Philippines, it is used as a diuretic.
-
How does it work?
Brahmi might increase certain brain chemicals that are involved in thinking, learning, and memory. Some research suggests that it might also protect brain cells from chemicals involved in Alzheimer’s disease.
Phase III trial of lupus drug Benlysta (belimumab) in patients with ANCA (Anti-neutrophil Cytoplasmic Antibodies) positive vasculitis
3 mar 2013
GSK, the company said it has kicked off a Phase III trial of its lupus drug Benlysta (belimumab) in patients with ANCA (Anti-neutrophil Cytoplasmic Antibodies) positive vasculitis, a condition characterised by inflammation of the blood vessels.
The multicentre, multi-national, randomised, double-blind study will assess the drug’s efficacy and safety in combination with azathioprine for the maintenance of remission in patients with a particular type of vascultitic disease called ANCA associated Vasculitis (Granulomatosis with Polyangiitis (Wegener’s) or microscopic polyangiitis).
Belimumab (trade name Benlysta, previously known as LymphoStat-B) is a human monoclonal antibody that inhibits B-cell activating factor (BAFF), also known as B-lymphocyte stimulator (BLyS) B cells are responsible for part of the normal immune response, and also for the over-aggressive immune response in autoimmune diseases like systemic lupus erythematosus (SLE).
Belimumab is approved in the United States, Canada and Europe for treatment of SLE. However, the major phase III trials excluded the more severe cases of SLE with kidney and brain damage, so its effectiveness has not been demonstrated in those cases. A Phase III study for SLE patients with kidney disease is now recruiting.
U.S. F.D.A. reviewers were concerned that belimumab is only “marginally” effective, and that there were more deaths in the treatment group.
Phase II trials of belimumab for rheumatoid arthritis were unsuccessful. Phase II trials for Sjögren’s Syndrome were more successful.
Belimumab was developed by Human Genome Sciences (HGS) and Cambridge Antibody Technology. GlaxoSmithKline acquired HGS, took belimumab through Phase III clinical trials, and markets belimumab.
Phase 3-Volasertib for acute myeloid leukaemia in patients ineligible for intensive induction therapy
Volasertib (BI 6727) for Acute myeloid leukaemia. is a cell cycle kinase inhibitor of polo-like kinases 1, 2 and 3. Volasertib inhibits cancer growth by disrupting cell division and inducing cell death. Volasertib is administered as a 350mg one hour intravenous (IV) infusion on days 1 and 15 of a 28 day cycle in combination with low-dose cytarabine (LDAC), administered via subcutaneous injection (SC) at 20mg twice daily on days 1-10 of a 28 day cycle.
Acute myeloid leukaemia (AML): previously untreated; patients considered ineligible for intensive remission induction therapy – first line; in combination with low-dose cytarabine
volasertib (also known as BI 6727) is a small molecule inhibitor of the PLK1 (polo-like kinase 1) protein being developed by Boehringer Ingelheim for use as an anti-cancer agent. Volasertib is the second in a novel class of drugs called dihydropteridinone derivatives.
FDA Approves Tris Pharma’s New Drug Application for Karbinal ER
Carbinoxamine Maleate
2-[p-Chloro-a-[2-(dimethylamino)ethoxy]benzyl]pyridine maleate (1:1) [3505-38-2].
April 3, 2013
Tris Pharma, a specialty pharmaceutical company focused on developing innovative drug delivery technologies, today announced that the U.S. Food and Drug Administration (FDA) has approved its New Drug Application (NDA) for Karbinal ER (carbinoxamine maleate) Extended-release Oral Suspension 4mg/5mL, the first sustained-release histamine receptor blocking agent indicated for the treatment of seasonal and perennial allergic rhinitis in children ages 2 and up.
“Karbinal ER is dosed only once every 12 hours, making it an attractive treatment option for the millions of allergy sufferers who don’t respond to second-generation antihistamines and aren’t satisfied with the cumbersome dosing schedules associated with the first-generation antihistamines,” said Ketan Mehta, founder, President, and CEO of Tris Pharma. “The approval of Karbinal ER marks our fourth liquid extended-release NDA approval based upon our proprietary OralXR+ technology. We are in the process of finalizing our marketing partner and plan to launch later this year in anticipation of the fall allergy season.”
Based on physician interviews approximately 30 percent of patients don’t get adequate relief from the non-sedating antihistamines. Carbinoxamine is a mildly-sedating antihistamine with years of proven safety and efficacy. Prior to 2006, carbinoxamine was widely used, with dozens of carbinoxamine-containing combination products including extended-release solid-dose products. However, nearly all of these were older products that hadn’t gone through the FDA’s rigorous approval process. Following the Drug Efficacy Study Implementation (DESI) review, the FDA removed all unapproved products with the exception of two immediate-release formulations, creating a void for patients and doctors who valued the benefits associated with an extended-release formulation.
Dr. Laura Garabedian, a New York-based pediatrician, said, “While I’ve always found carbinoxamine to be an effective option for treating the symptoms of allergies in children, the existing immediate-release formulations of carbinoxamine require dosing multiple times a day. This is especially inconvenient for children who are in school. Now, with the approval of Karbinal ER, I look forward to having an effective and great-tasting extended-release liquid formulation to offer patients as young as two years old.”
Karbinal ER Extended-release Oral Suspension is an H1 receptor antagonist indicated for the symptomatic treatment of:
- Seasonal and perennial allergic rhinitis
- Vasomotor rhinitis
- Allergic conjunctivitis due to inhalant allergens and foods
- Mild, uncomplicated allergic skin manifestations of urticaria and angioedema
- Dermatographism
- As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled
- Amelioration of the severity of allergic reactions to blood or plasma
Tris Pharma is a specialty pharmaceutical company focused on the research and development of technologies-driven products. Tris has pioneered the delivery of sustained release in the liquid, chewable/ODT and strip dosage forms so patients do not have to swallow a pill. Tris’ Nobuse™ technology provides abuse deterrence for opioids and other abuse-prone drugs. Tris’ R&D and manufacturing facilities are located in Monmouth Junction, New Jersey, U.S.A. For more information, please visit http://www.trispharma.com.
Drug spotlight-Raloxifene
Raloxifene
Raloxifene: The FDA approved Raloxifene to reduce the risk of invasive breast cancer in postmenopausal women in 2007. It was initially developed to treat osteoporosis.
| Identifiers | |
|---|---|
| CAS number | 84449-90-1 |
Raloxifene (marketed as Evista by Eli Lilly and Company) is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women.
In 2006, the National Cancer Institute announced that raloxifene was as effective astamoxifen in reducing the incidence of breast cancer in postmenopausal women at increased risk. A major adverse effect of tamoxifen is uterine cancer; raloxifene had fewer uterine cancers. Tamoxifen increased the risk of cataracts, but raloxifene did not. Both groups had more blood clots in veins and the lungs, but that side effect was more common with tamoxifen than raloxifene.[2][3][4] On September 14, 2007, the U.S. Food and Drug Administration announced approval of raloxifene for reducing the risk of invasive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women at high risk for invasive breast cancer.[5]
An editorial in Lancet Oncology criticized the way that information about the drug was released.[6]
Raloxifene hydrochloride (HCl) has the empirical formula C28H27NO4S•HCl, which corresponds to a molecular weight of 510.05 g/mol. Raloxifene HCl is an off-white to pale-yellow solid that is slightly soluble in water.
SERMs mimic estrogen in some tissues and have anti-estrogen activity in others. Other SERMs, such as Pfizer’s lasofoxifene and Wyeth’s bazedoxifene are in the later development phases.
Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausalwomen, for reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. For either osteoporosis treatment or prevention, supplemental calciumand/or vitamin D should be added to the diet if daily intake is inadequate.
Raloxifene is contraindicated in lactating women or women who are or may becomepregnant, in women with active or past history of venous thromboembolic events, includingdeep vein thrombosis, pulmonary embolism, and retinal vein thrombosis and in women known to be hypersensitive to raloxifene.
Common adverse events considered to be drug-related were hot flashes and leg cramps.
Raloxifene may infrequently cause serious blood clots to form in the legs, lungs, or eyes. Other reactions experienced include leg swelling/pain, trouble breathing, chest pain, vision changes. Raloxifene is a teratogenic drug, i.e., can cause developmental abnormalities such as birth defects.
In a 2006 study published in New England Journal of Medicine, raloxifene produced significantly more strokes and blood clots than the placebo.[7]
A report in September 2009 from Health and Human Services’ Agency for Healthcare Research and Quality suggests that tamoxifen and raloxifene, used to treat breast cancer significantly reduce invasive breast cancer in midlife and older women, but also increase the risk of adverse side effects.[8]
As cancer drug
Bottle of Raloxifene
Raloxifene reduces the risk of hormone-positive breast cancer and vertebral fractures “without a shadow of a doubt,” but its effects on cardiovascular disease remain less certain, according to the results of the “Raloxifene for Use of the Heart” (RUTH) study published in the July 13, 2006 issue of the New England Journal of Medicine by Dr. Elizabeth Barrett-Connor (University of California at San Diego) and colleagues.[9]
In the trial, in women with coronary heart disease (CHD) or multiple risk factors for CHD, raloxifene had no significant effect on the primary end point, coronary events, but it did significantly increase the risk of venous thromboembolism (VTE). And although the drug had no effect on stroke, there was a seemingly paradoxical significant increase in death from stroke.[10]
On September 14, 2007, Steven K. Galson, the director of the United States Food and Drug Administration’s Center for Drug Evaluation and Research announced authorization of the sale of raloxifene to prevent invasive breast cancer in post-menopausal women.[11]
Chemical synthesis
Jones, Charles D.; Jevnikar, Mary G.; Pike, Andrew J.; Peters, Mary K.; Black, Larry J.; Thompson, Allen R.; Falcone, Julie F.; Clemens, James A. (1984). “Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-[4-[2-(1-piperidinyl)ethoxy]phenyl]methanone hydrochloride (LY 156758), a remarkably effective estrogen antagonist with only minimal intrinsic estrogenicity”. Journal of Medicinal Chemistry 27 (8): 1057–66.doi:10.1021/jm00374a021. PMID 6431104.
- Jeong, Eun Ju; Liu, Yong; Lin, Huimin; Hu, Ming (2005-03-15). “Species- and Disposition Model-Dependent Metabolism of Raloxifene in Gut and Liver: Role of UGT1A10”. Drug Metabolism and Disposition ( ASPET) 33 (6): 785–794. doi:10.1124/dmd.104.001883.PMID 15769887. Retrieved 2010-10-20.
- Study of Tamoxifen and Raloxifene (STAR) Trial Cancer.gov
- Results of the Study of Tamoxifen and Raloxifene (STAR) Released: Osteoporosis Drug Raloxifene Shown to be as Effective as Tamoxifen in Preventing Invasive Breast Cancer (Press Release) 06/21/2006
- Vogel, Victor; Joseph Constantino, Lawrence Wickerman et al. (2006-06-21). “Effects of Tamoxifen vs. Raloxifene on the Risk of Developing Invasive Breast Cancer and Other Disease Outcomes”. The Journal of the American Medical Association 295 (23): 2727–2741. doi:10.1001/jama.295.23.joc60074. PMID 16754727.
- “FDA Approves New Uses for Evista” (Press release). U.S. Food and Drug Administration. 2007-09-14. Retrieved 2007-09-15.
- Thelancetoncology, (2006). “A STARring role for raloxifene?”. Lancet Oncol 7 (6): 443. doi:10.1016/S1470-2045(06)70701-X.PMID 16750489.
- 355:125-137 July 13, 2006, Effects of Raloxifene on Cardiovascular Events and Breast Cancer in Postmenopausal Women Elizabeth Barrett-Connor, Lori Mosca, Peter Collins, et al. for the Raloxifene Use for The Heart (RUTH) Trial Investigators [Free full text]
- OncoGenetics.Org (September 2009). “Medications Effective in Reducing Risk of Breast Cancer But Increase Risk of Adverse Effects”. OncoGenetics.Org. Retrieved 2009-09-14.[dead link]
- Lisa Nainggolan (July 12, 2006). A balancing act: The pro and cons of raloxefene.
- Barrett-Connor E, Mosca L, Collins P, et al. (2006-07-13). “Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women”. New England Journal of Medicine 355 (2): 125–137. doi:10.1056/NEJMoa062462. PMID 16837676.
- AFP.google.com, US approves Lilly’s Evista for breast cancer prevention
- STAR: a head-to-head comparison of tamoxifen and raloxifene as breast-cancer preventatives
- Full Prescribing Information
- Position paper of the National Women’s Health Network
- Heringa M (2003). “Review on raloxifene: profile of a selective estrogen receptor modulator”. Int J Clin Pharmacol Ther 41 (8): 331–45. PMID 12940590.
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Dr. Reddy’s launches Zenatane (Isotretinoin Capsules USP) in US
Isotretinoin
1 APRIL, 2013
India-based Dr. Reddy’s Laboratories has announced the launch of Zenatane (Isotretinoin Capsules USP) in 20mg and 40mg strengths in the US.
The launch follows the FDA approval of the company’s ANDA for Zenatane 10mg, 20mg and 40mg.
Zenatane (Isotretinoin Capsules USP) is a generic version, therapeutically equivalent to Accutane (Isotretinoin Capsules USP).
Isotretinoin is indicated for the treatment of severe recalcitrant nodular acne.
The company is making the product available in 10mg, 20mg, and 40mg strengths in boxes of 30 as unit dose blisters.
Isotretinoin, first marketed as Accutane byHoffmann-La Roche, is a medication used mostly for cystic acne. It is also achemotherapy treatment used in brain, pancreatic and other cancers. It is used to treat harlequin-type ichthyosis, a usually lethal skin disease, and lamellar ichthyosis. Its effects are systemic and nonselective. It is a retinoid, meaning it is related to vitamin A, and is found in small quantities naturally in the body.
Isotretinoin’s best-known and most dangerous side effect is birth defects due to in utero exposure. This is because of the molecule’s close resemblance to retinoic acid, a natural vitamin A derivative which controls normal embryonic development. In the United States a special procedure is required to obtain the pharmaceutical (see below).
In 2009, Roche decided to pull Accutane off the US market after juries had awarded millions of dollars in damages to former Accutane users over inflammatory bowel disease claims. Among others, actor James Marshall sued Roche over Accutane-related disease that resulted in removal of his colon.
The most common brands are Roaccutane (Hoffman-La Roche, known as Accutane in the United States before July 2009), Amnesteem (Mylan), Claravis (Barr), Isotroin(Cipla) or Sotret (Ranbaxy).
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