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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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FDA Approves Diclegis for Pregnant Women Experiencing Nausea and Vomiting
doxylamine
pyridoxine
8 april 2013
The U.S. Food and Drug Administration today approved Diclegis (doxylamine succinate and pyridoxine hydrochloride) to treat pregnant women experiencing nausea and vomiting. Diclegis is a delayed-release tablet intended for women who have not adequately responded to conservative management of nausea and vomiting during pregnancy, such as dietary and lifestyle modifications.
These modifications include eating several small meals instead of three large meals, eating bland foods that are low in fat and easy to digest and avoiding smells that can trigger nausea. “Many women experience nausea and vomiting during pregnancy, and sometimes these symptoms are not adequately managed through recommended changes in diet and lifestyle,” said Hylton V. Joffe, M.D., M.M.Sc., director of the Division of Reproductive and Urologic Products in the FDA’s Center for Drug Evaluation and Research.
“Diclegis is now the only FDA-approved treatment for nausea and vomiting due to pregnancy, providing a therapeutic option for pregnant women seeking relief from these symptoms.” Diclegis was studied in 261 women experiencing nausea and vomiting due to pregnancy. Study participants in the clinical trial were at least 18 years old and had been pregnant for at least 7 weeks and up to 14 weeks. Women were randomly assigned to receive two weeks of treatment with Diclegis or a placebo.
The study results showed that women taking Diclegis experienced greater improvement in nausea and vomiting than those taking placebo. Additionally, observational (epidemiological) studies have shown that the combination of active ingredients in Diclegis does not pose an increased risk of harm to the fetus. Diclegis is taken daily. Tablets must be taken whole on an empty stomach. The recommended starting dose is two tablets taken at bedtime.
If symptoms are not adequately controlled, the dose can be increased to a maximum recommended dose of four tablets daily (one in the morning, one mid-afternoon and two at bedtime). Nausea and vomiting due to pregnancy usually improve after the first trimester. Health care professionals should reassess their patients for continued need for Diclegis as pregnancy progresses. Drowsiness or sleepiness, which can be severe, is the most common side effect reported by women taking Diclegis.
Women should avoid using Diclegis when engaging in activities requiring mental alertness, such as driving or operating heavy machinery, until cleared to do so by their health care provider.
Diclegis is marketed by Duchesnay Inc., based in Blainville, Québec, Canada.
AURVEDA-Shatavari, wonder herb for women’s overall health and vitality .
Asparagus racemosus (Satavar, Shatavari, or Shatamull) is a species of asparagus common throughout Sri Lanka, India and the Himalayas. It grows one to two metres tall and prefers to take root in gravelly, rocky soils high up in piedmont plains, at 1,300–1,400 metres elevation).It was botanically described in 1799. Due to its multiple uses, the demand for Asparagus racemosus is constantly on the rise. Due to destructive harvesting, combined with habitat destruction, and deforestation, the plant is now considered ‘endangered’ in its natural habitat.
Asparagus racemosus (Shatavari) is recommended in Ayurvedic texts for the prevention and treatment of gastric ulcers, dyspepsia and as a galactogogue. A. racemosus has also been used successfully by some Ayurvedic practitioners for nervous disorders.
Shatawari has different names in the different Indian languages, such as Shatuli, Vrishya and other terms. In Nepal it is called Kurilo. The name Shatawari means “curer of a hundred diseases” (shat: “hundred”; vari: “curer”).
Shatavari is mentioned under six important rasayanas in ayurveda. Rasayanas are those plant drugs which promote general well being of an individual by increasing cellular vitality or resistance. This bitter sweet herb is especially used in Ayurveda to correct Pitta dosha imbalance.
Shatavari: This powerful herb strengthens the female organs, enhancing fertility and sexual vitality. Works on the reproductive, respiratory, circulatory and digestive systems. Excellent herb to cool Pitta and to bring moisture and lustre to the skin, while nourishing the cells and tissues. Shatavari soothes and protects the dry and inflamed membranes of the lungs, stomach, kidneys and sexual organs. Found in our Pitta spicebodhi herbal body bar and our spicebodhimama massage oil.
Asparagamine A, a polycyclic alkaloid with antitumor activity against a variety of cell lines was isolated from the dried roots and subsequently synthesized to allow for the construction of analogs.
Two new steroidal saponins, shatavaroside A and shatavaroside B together with a known saponin, filiasparoside C, were isolated from the roots of Asparagus racemosus.
Five steroidal saponins, shatavarins VI-X, together with five known saponins, shatavarin I (or asparoside B), shatavarin IV (or asparinin B), shatavarin V, immunoside and schidigerasaponin D5 (or asparanin A), have been isolated from the roots of Asparagus racemosus.
Isoflavone, 8-methoxy-5,6,4′-trihydroxyisoflavone 7-O-beta-D-glucopyranoside
Asparagus racemosus is an important medicinal plant of tropical and subtropical India. Its medicinal usage has been reported in the Indian and British Pharmacopoeias and in traditional systems of medicine such as Ayurveda, Unani and Siddha. It is mainly known for its phytoestrogenic properties. In Ayurveda, Asparagus racemosus has been described as a rasayana herb and has been used extensively as an adaptogen to increase the non-specific resistance of organisms against a variety of stresses. Besides use in the treatment of diarrhoea and dysentery, the plant also has antioxidant, immunostimulant, anti-dyspepsia and antitussive effects.”
The roots are used in Ayurvedic medicine, following a regimen of processing and drying. It is generally used as a uterine tonic, as agalactogogue (to improve breast milk), in hyperacidity, and as a general health tonic.
The reputed adaptogenic effects of Shatavari may be attributed to its concentrations of saponins,known as Shatavarins.
conclusion
Shatavari or Asparagus racemosus is a popular herb aptly called the “Female Health Formula”. Asparagus racemosus is the most commonly used Asparagus species in ayurveda and indigenous medicine in India. The plant is called shatawar in Hindi and in Sanskrit this plant is called shatavari which means ‘able to have one hundred husbands’. In Ayurveda this amazing herb is known as the “queen of herbs” because it promotes love and positive emotions and is very useful in strengthening the reproductive system of women. It is also a very important herb for women’s overall health and vitality
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Pharmacyclics Announces Third Breakthrough Therapy Designation for Ibrutinib from the U.S. Food and Drug Administration
IBRUTINIB
1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
SUNNYVALE, Calif., April 8, 2013
Pharmacyclics, Inc. announced today that the U.S. Food and Drug Administration (FDA) has granted an additional Breakthrough Therapy Designation for the investigational oral agent ibrutinib as monotherapy for the treatment of chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) patients with deletion of the short arm of chromosome 17 (deletion 17p). Patients harboring a deletion within chromosome 17 generally have poor response to chemoimmunotherapy and have limited treatment options. The presence of deletion 17p is one of the worst prognostic factors in patients with CLL.
In February 2013, FDA granted Breakthrough Therapy Designations for ibrutinib as a monotherapy for the treatment of patients with relapsed or refractory mantle cell lymphoma (MCL) and as a monotherapy for the treatment of patients with Waldenstrom’s macroglobulinemia (WM), both of which are also B-cell malignancies. Ibrutinib is jointly being developed by Pharmacyclics and Janssen for treatment of B-cell malignancies.
The Breakthrough Therapy Designation is intended to expedite the development and review of a potential new drug for serious or life-threatening diseases where “preliminary clinical evidence indicates that the drug may demonstrate substantial improvement over existing therapies on one or more clinically significant endpoints, such as substantial treatment effects observed early in clinical development.” The designation of a drug as a Breakthrough Therapy was enacted as part of the 2012 Food and Drug Administration Safety and Innovation Act. Pharmacyclics, together with Janssen, is working with the FDA to determine the implications of this Breakthrough Therapy Designation to the ongoing and planned development and the FDA filing requirements for the use of ibrutinib in CLL patients with deletion 17p.
The FDA Breakthrough Therapy Designation for ibrutinib in CLL patients with deletion 17p was based on data from pre-clinical and clinical studies where ibrutinib as a monotherapy was used to treat patients with this disease. Ibrutinib has the potential to improve the outcome in this serious and life-threatening disease which has a poor prognosis. In addition, Pharmacyclics and Janssen have recently initiated a Phase II study of ibrutinib in patients with CLL deletion 17p, RESONATE™ -17, which is a single-arm, open-label, multi-center trial using ibrutinib as a monotherapy in patients who have deletion 17p and who did not respond to or relapsed after at least one prior CLL treatment (a high unmet need population). The primary endpoint of the study will be overall response rate. This global study opened this year and Pharmacyclics plans to enroll 111 patients worldwide.
About Chronic Lymphocytic Leukemia
Chronic Lymphocytic Leukemia (CLL) is a slow-growing blood cancer that starts in the white blood cells (lymphocytes), most commonly from B-cells. CLL is the second most common adult leukemia. Approximately 16,000 patients in the US are diagnosed each year with CLL. The prevalence of CLL is approximately 113,000 in the US. The disease is a chronic disease of the elderly with an average survival of about 5 years. Patients commonly receive multiple lines of treatment over the course of their disease.
In CLL the genetic mutation 17p deletion occurs when the short arm of chromosome 17 is missing. Del 17p is associated with abnormalities of a key tumor suppressor gene, TP53, which results in poor response to chemoimmunotherapy and worse treatment outcomes. It occurs in about 7% of treatment naive CLL patients and is estimated to be approximately 20% to 40% of relapsed or refractory patients harboring the mutation.
About Ibrutinib
Ibrutinib , previously publicly known as PCI-32765, is an experimental drug candidate for the treatment of various types of cancer. It was first synthesized at Celera Genomics as a selective inhibitor of Bruton’s tyrosine kinase (Btk).It was later discovered to have anti-lymphoma properties in vivo by scientists at Pharmacyclics, Inc.Ibrutinib is currently under development by Pharmacyclics, Inc and Johnson & Johnson‘sJanssen Pharmaceutical division for chronic lymphocytic leukemia, mantle cell lymphoma,diffuse large B-cell lymphoma, and multiple myeloma. It also has potential effects against autoimmune arthritis.
Janssen Biotech, Inc. and Pharmacyclics entered a collaboration and license agreement in December 2011 to co-develop and co-commercialize ibrutinib. Ibrutinib was designed to specifically target and selectively inhibit an enzyme called Bruton’s tyrosine kinase (BTK). BTK is a key mediator of at least three critical B-cell pro-survival mechanisms occurring in parallel – regulation of apoptosis, adhesion, and cell migration and homing. Through these multiple signals, BTK regulation helps to direct malignant B-cells to lymphoid tissues, thus allowing access to a micro environment necessary for survival.
The effectiveness of ibrutinib alone or in combination with other treatments is being studied in several B-cell malignancies, including chronic lymphocytic leukemia/small lymphocytic lymphoma, mantle cell lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, Waldenstrom’s macroglobulinemia and multiple myeloma. To date five Phase III trials have been initiated with ibrutinib and a total of 26 trials are currently registered on www.clinicaltrials.gov.
About Pharmacyclics
Pharmacyclics® is a clinical-stage biopharmaceutical company focused on developing and commercializing innovative small-molecule drugs for the treatment of cancer and immune mediated diseases. Our mission and goal is to build a viable biopharmaceutical company that designs, develops and commercializes novel therapies intended to improve quality of life, increase duration of life and resolve serious unmet medical healthcare needs; and to identify promising product candidates based on scientific development and administrational expertise, develop our products in a rapid, cost-efficient manner and pursue commercialization and/or development partners when and where appropriate.
Presently, Pharmacyclics has three product candidates in clinical development and several preclinical molecules in lead optimization. The Company is committed to high standards of ethics, scientific rigor, and operational efficiency as it moves each of these programs to viable commercialization.
The Company is headquartered in Sunnyvale, California and is listed on NASDAQ under the symbol PCYC. To learn more about how Pharmacyclics advances science to improve human healthcare visit at http://www.pharmacyclics.com.
FDA Extends Delcath’s Melblez Cancer System Review
Melphalan hydrochloride (trade name Alkeran) is a chemotherapy drug belonging to the class of nitrogen mustard alkylating agents.
An alkylating agent adds an alkyl group (CnH2n+1) to DNA. It attaches the alkyl group to the guanine base of DNA, at the number 7 nitrogen atom of the imidazole ring.
Otherwise known as L-Phenylalanine Mustard, or L-PAM, melphalan is a phenylalaninederivative of mechlorethamine.
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.
New combination therapy cures patient with advanced ovarian cancer
A novel ovarian cancer treatment made from tumour cells has cured a woman in the US with an advanced form of the disease, scientists at the Perelman School of Medicine at the University of Pennsylvania have announced.
During a preliminary trial of the two-step immunotherapy, the patient achieved complete remission, while seven other women had no measurable disease at the end of the study.
The therapy includes a personalised immune cell vaccination made from the patients’ live tumour cells and adoptive T-cell therapy.
Both treatments are given in conjunction with Avastin (bevacizumab), a drug developed by Roche that controls the blood vessel growth that feeds tumours.
The second step in the study involved the isolation of immune cells, known as dendritic cells, from the patients’ blood through a process called apheresis, similar to the process used for blood donation.
Announcing its findings at the American Association of Cancer Research (AACR) Annual Meeting in Washington DC on Saturday, the research team reported that in the study of 31 patients, vaccination therapy alone showed a 61% clinical benefit, and the combination of both therapies benefited around 75% of participants.
Ovarian cancer is the fifth leading cause of cancer-related deaths among women in the US, taking the lives of 14,000 people each year.
Lead author of the study Lana Kandalaft said; “Given these grim outcomes, there is definitely a vast unmet need for the development of novel, alternate therapies.”
“This is the first time such a combination immunotherapy approach has been used for patients with ovarian cancer, and we believe the results are leading us toward a completely new way to treat this disease.”
The vaccine trial is still open to accrual to test new combinatorial strategies.
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.
DRUG SPOTLIGHT – HALOPERIDOL
HALOPERIDOL
CAS No:- [52-86-8]
IUPAC Name:- 4-[4-(4-Chlorophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)-1-butanone
MW: 375.86, C21H23ClFNO2
Drug information:- Haloperidol is an anti-psychotic drug. This butyrophenone compound is used for the treatment of schizophrenia and other psychotic disorders in adults and childrens.
Haloperidol was discovered by Paul Janssen. It was developed in 1958 at the Belgian company Janssen Pharmaceutica and submitted to the first of clinical trials in Belgium later that year.
Haloperidol was approved by the U.S. Food and Drug Administration (FDA) on April 12, 1967; it was later marketed in the U.S. and other countries under the brand name Haldol by McNeil Laboratories.
Haloperidol is a dopamine inverse agonist of the typical antipsychotic class of medications. It is a butyrophenone derivative and has pharmacological effects similar to the phenothiazines.
Haloperidol is an older antipsychotic used in the treatment of schizophrenia and acutepsychotic states and delirium. A long-acting decanoate ester is used as an injection given every four weeks to people with schizophrenia or related illnesses who have poor adherence to medication regimens and suffer frequent relapses of illness, or to overcome the drawbacks inherent to its orally administered counterpart that burst dosage increases risk or intensity of side effects. In some countries, such as the United States of America, injections of antipsychotics such as haloperidol can be ordered by a court at the request of a psychiatrist.
Haloperidol is sold under the tradenames Aloperidin, Bioperidolo, Brotopon, Dozic,Duraperidol (Germany), Einalon S, Eukystol, Haldol (common tradename in the US and UK), Halosten, Keselan, Linton, Peluces, Serenace, Serenase, andSigaperidol
Conditions:-
i. Fluorobenzene, aluminum chloride, carbon disulfide, room temperature, 2 h,
ii. 4-(p-chlorophenyl)piperadine-4-ol, potassium iodide, toluene, 100 – 110 ºC
Arena Pharmaceuticals Initiates Phase 1 Clinical Trial of APD334 for Autoimmune Diseases
April 5, 2013
Arena Pharmaceuticals, Inc. announced today the initiation of dosing in a Phase 1 clinical trial of APD334, a novel oral drug candidate that targets the sphingosine 1-phosphate subtype 1 (S1P1) receptor for the potential treatment of autoimmune diseases.
This randomized, double-blind and placebo-controlled Phase 1 trial will evaluate the safety, tolerability and pharmacokinetics of single-ascending doses of APD334 in up to 64 healthy adult volunteers.
“We are pleased to expand our clinical-stage pipeline by initiating a Phase 1 trial of APD334, and look forward to advancing this novel compound through our validated development platform,” said William R. Shanahan, M.D., Arena’s Senior Vice President and Chief Medical Officer. “APD334’s selectivity for the S1P1 receptor has the potential to improve upon the adverse event profile of currently available treatments for a spectrum of autoimmune diseases.”
About Autoimmune Diseases
Autoimmune diseases are characterized by an inappropriate immune response against substances and tissues that are normally present in the body. In an autoimmune reaction, a person’s antibodies and immune cells target healthy tissues, triggering an inflammatory response. Reducing the immune and/or inflammatory response is an important goal in the treatment of autoimmune disease.
About APD334
APD334 is an orally available drug candidate discovered by Arena that targets the S1P1 receptor for the potential treatment of a number of conditions related to autoimmune diseases, including multiple sclerosis, psoriasis and rheumatoid arthritis. S1P1 receptors have been demonstrated to be involved in the modulation of several biological responses, including lymphocyte trafficking from lymph nodes to the peripheral blood. By isolating lymphocytes in lymph nodes, fewer immune cells are available in the circulating blood to effect tissue damage. Arena has optimized APD334 as a potent and selective small molecule S1P1 receptor agonist that reduces the severity of disease in preclinical autoimmune disease models.
About Arena Pharmaceuticals
Arena is a biopharmaceutical company focused on discovering, developing and commercializing novel drugs that target G protein-coupled receptors, or GPCRs, to address unmet medical needs. BELVIQ® (lorcaserin HCl), Arena’s internally discovered drug, was approved by the US Food and Drug Administration in June 2012 and is under review for regulatory approval in additional territories. Arena’s US operations are located in San Diego, California, and its operations outside of the United States, including its commercial manufacturing facility, are located in Zofingen, Switzerland. For more information, visit Arena’s website at www.arenapharm.com.
Arena Pharmaceuticals® and Arena® are registered service marks of Arena Pharmaceuticals, Inc. BELVIQ® is a registered trademark of Arena Pharmaceuticals GmbH
New Drug Approvals 