DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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(sNDA)…..FDA okays Shire ADHD drug Vyvanse (lisdexamfetamine dimesylate) for binge eating
Yet more good news for Shire has come with the US Food and Drug Administration approving its attention-deficit hyperactivity disorder blockbuster Vyvanse for binge-eating disorder, the first medicine approved by the agency to treat this condition.
The agency has expanded approval on Vyvanse (lisdexamfetamine dimesylate) for adults with BED based on two Phase III studies which showed that it was statistically superior to placebo in terms of number of binge days per week. BED affects around 2.8 million US adults and is more prevalent than anorexia nervosa and bulimia nervosa combined.
Read more at: http://www.pharmatimes.com/Article/15-01-30/FDA_okays_Shire_ADHD_drug_Vyvanse_for_binge_eating.aspx
Originally discovered and developed by New River Pharmaceuticals, the company entered into a collaborative agreement with Shire Pharmaceuticals in 2005 for global commercialization of the drug candidate. After Shire’s acquisition of New River Pharmaceuticals in April 2007, lisdexamfetamine entered the product portfolio of Shire.
In 2009, the compound was licensed to GlaxoSmithKline by Shire in the U.S. for comarketing for the treatment of attention deficit/hyperactivity disorder (ADHD). In 2010, this license agreement was terminated. The product was licensed to Shionogi by Shire in Japan for co-development, co-commercialization, and co-promotion for the treatment of attention deficit/hyperactivity disorder (ADHD).
Lisdexamfetamine (NRP-104), a conditionally bioreversible derivative of amphetamine, was launched in the U.S. in 2007 for the treatment of attention deficit hyperactivity disorder (ADHD) in children aged 6-12 years old. In 2008, the product was approved for use in adults, and in 2009 it was approved in Canada, followed by commercialization in 2010. In 2010, FDA approval was obtained for use in treatment of ADHD in adolescents aged 13 to 17 years and launch took place the same year. Approval for the treatment of adolescents was assigned in Canada in 2011.
In 2012, Shire filed a regulatory application in Europe via the decentralized procedure with the U.K. acting as the reference member state, for the treatment of ADHD in children and adolescent patients aged 6 to 17 years. This indication was approved in 2013. Also, in 2012 FDA approval was granted for the maintenance treatment for adults with ADHD. U.K., DK and SE are awaiting approval for the same indication in a decentralized procedure initiated in 2014 with the U.K. acting as the reference member state. In 2014, the company filed with priority review a supplemental New Drug Application (sNDA) in the U.S. for the treatment binge eating in adults.
cas 608137-33-3
(2S)-2,6-Diamino-N-[(1S)-1-methyl-2-phenylethyl]hexanamide dimethanesulfonate
Binge eating,,,,,, express their stress as temper tantrums or by indulging in compulsive eating spree
In terms of clinical development, phase III clinical trials are ongoing at Shionogi in Japan for the treatment of ADHD.. The National Institute on Drug Abuse (NIDA) is evaluating the compound in early clinical studies for the treatment of methamphetamine dependence. Phase III trials were underway as an adjunctive treatment of major depressive disorder; however, they were discontinued due to lack of efficacy. A phase II clinical trial for the treatment of excessive daytime sleepiness (EDS) has been completed. Shire had been evaluating the compound in clinical studies for the treatment of chronic fatigue syndrome.
In 2013, Shire cancelled its phase III program evaluating the product for the negative symptoms of schizophrenia based on a review and prioritization of the company’s development portfolio.
http://www.google.co.in/patents/US7662787
RIVER PHARMA
Patent and Exclusivity Search Results from query on Appl No 021977 Product 003 in the OB_Rx list.
Patent Data
| Appl No | Prod No | Patent No | Patent Expiration |
Drug Substance Claim |
Drug Product Claim |
Patent Use Code |
Delist Requested |
|---|---|---|---|---|---|---|---|
| N021977 | 003 | 7105486 | Jun 29, 2023 | U – 727 | |||
| N021977 | 003 | 7223735 | Jun 29, 2023 | Y | |||
| N021977 | 003 | 7655630 | Feb 24, 2023 | Y | |||
| N021977 | 003 | 7659253 | Feb 24, 2023 | Y | Y | U – 727 | |
| N021977 | 003 | 7659254 | Feb 24, 2023 | U – 1034 | |||
| N021977 | 003 | 7662787 | Feb 24, 2023 | Y | |||
| N021977 | 003 | 7662788 | Feb 24, 2023 | U – 727 | |||
| N021977 | 003 | 7671030 | Feb 24, 2023 | Y | U – 727 | ||
| N021977 | 003 | 7671031 | Feb 28, 2023 | U – 727 | |||
| N021977 | 003 | 7674774 | Mar 18, 2023 | Y | U – 842 | ||
| N021977 | 003 | 7678770 | Mar 25, 2023 | U – 842 | |||
| N021977 | 003 | 7678771 | Mar 25, 2023 | Y | U – 842 | ||
| N021977 | 003 | 7687466 | Feb 24, 2023 | Y | |||
| N021977 | 003 | 7687467 | Apr 8, 2023 | Y | U – 842 | ||
| N021977 | 003 | 7700561 | Jun 29, 2023 | Y | |||
| N021977 | 003 | 7713936 | Feb 24, 2023 | U – 727 | |||
| N021977 | 003 | 7718619 | Feb 24, 2023 | Y | U – 842 | ||
| N021977 | 003 | 7723305 | Feb 24, 2023 | Y | U – 842 |
Exclusivity Data
| Appl No | Prod No | Exclusivity Code | Exclusivity Expiration |
|---|---|---|---|
| N021977 | 003 | I – 645 | Jan 31, 2015 |
Lead-oriented synthesis: a new concept to aid drug-discovery process
Figure 2. a. Fragment-based screening: Small and structurally diverse molecules (circles represent functional groups) are screened for a biological target, and they are combined and modified to generate drug-like compounds. b. Diversity-oriented synthesis: Large collections of structurally diverse and complex molecules are made using a short number of reactions. The resulting compounds are optimized to produce the drug-like compounds. | Credit: P. J. Hajduk,W. R. J. D. Galloway & D. R. Spring Nature, 2011, 470, 42–43. DOI: 10.1038/470042a
The discovery and development of new drugs is a long and expensive process, and despite of it, essential to face present and new diseases. For small molecules, which account for the majority of the marketed drugs, the discovery process generally involves finding a starting point termed hit or lead compound. These molecules have biological activity but need to be optimized to enhance their potency and selectivity (i.e. minimize the toxicity) and improve pharmacokinetic parameters making them suitable to go to the next stage, the pre-clinical tests……….http://mappingignorance.org/2014/07/04/lead-oriented-synthesis-new-concept-aid-drug-discovery-process/
Author
pablo ortiz
PhD at Rijksuniversiteit Groningen
Experience
PhD Student, Rijksuniversiteit Groningen
October 2013 – Present
Asymmetric organometallic catalysis focused on tertiary alcohols and amines
Harutyunyan research group
Master Thesis Project
University of the Basque Country
February 2013 – September 2013 (8 months)Vitoria-Gasteiz Area, Spain
Estereoselective synthesis of quaternary alpha-aminophosphonic acid derivatives (organocatalysis)
Locum pharmacist
Community pharmacy
August 2012 – August 2012 (1 month)La Rioja, Spain
Pre-registration pharmacist
NHS Trust
January 2012 – June 2012 (6 months)Southport, England
In-patient and out-patient dispensing
Clinical pharmacy
Medicines information
Anticoagulant management
Aseptic preparation of medicines
Clinical audit of antimicrobial use
Publications
Tertiary α-diarylmethylamines derived from diarylketimines and organomagnesium reagents(Link)
Chem. Commun. 2015, 51, 703-706.
November 13, 2014
Organomagnesium reagents enable swift and versatile derivatisation of diarylimines to the corresponding α-substituted diarylmethylamines in excellent yields, through fast and clean reactions. Where it occurs, 1,2-reduction can be circumvented using readily accessible dialkylmagnesium reagents.
Asymmetric Synthesis of Functionalized Tetrasubstituted α-Aminophosphonates through Enantioselective Aza-Henry Reaction of Phosphorylated Ketimines(Link)
J. Org. Chem., 2015, 80, 156–164
November 2014
Bifunctional Cinchona alkaloid thioureas efficiently catalyze asymmetric nucleophilic addition of nitromethane to ketimines derived from α-aminophosphonic acids to afford tetrasubstituted α-amino-β-nitro-phosphonates.
Catalytic Asymmetric Alkylation of Aryl Heteroaryl Ketones(Link)
Eur. J. Org. Chem., 2015, 72–76.
November 2014
Tertiary diarylmethanols are highly bioactive structural motifs. A new strategy to access chiral tertiary diarylmethanols through copper-catalyzed direct alkylation of (di)(hetero)aryl ketones by using Grignard reagents was developed. The low reactivity and the similarity of the enantiotopic faces of bis-aromatic ketones were partially overcome, which resulted in moderate to good yields and…more
Synthesis of Tetrasubstituted α-Aminophosphonic Acid Derivatives from Trisubstituted α-Aminophosphonates(Link)
Eur. J. Org. Chem., 2013: 7095–7100
September 2013
Education
Universidad del País Vasco/Euskal Herriko Unibertsitatea
Master’s degree, Synthetic and Industrial Chemistry, 9.2
2012 – 2013
- (Open)1 course
Universidad del País Vasco/Euskal Herriko Unibertsitatea
Bachelor’s degree, Pharmacy, Extraordinary Degree Award, 9.06
2007 – 2012
- (Open)1 honor or award
- (Open)2 courses
Courses
Universidad del País Vasco/Euskal Herriko Unibertsitatea
- How to write and publish a research article
- X Pharmaceutical Chemistry Sessions: New strategies for the design and synthesis of drugs
Universidad del País Vasco/Euskal Herriko Unibertsitatea
- II Organic Chemistry Synthesis and Catalysis Workshop: Methods and strategies in synthesis
GRONINGEN, NETHERLANDS
stadtmitte groningen niederlande stadtwanderung
AYURVEDA……..Dronapushpi (দ্রোনপুষ্পি)
Dronapushpi is Sanskrit name of plant Leucas cephalotes. It is a medicinal herb that grows as a weed in India and many South East Asian countries. The folk use of this herb is for treating scorpion stings, snake bite, cough, fever etc. The whole plant has fever educing and insecticidal properties. The leaves are applied externally on snake bites and scorpion stings. To know more about this medicinal herb,
‘Leucas aspera ‘
SYNONYMS
- Ksavapatra
- Chatrini
- Palepushpa
- Guma
- Nahula
- Adhicchatra
- Dvesyamesa
- Gotamah
- Putigandhika
- Kumbhayoni
- Kutumbaka
- Drona
- Swasanaka
- Palindi
- Chatrani
- Chatraka
- Koodinya
- Vrakshasaraka
- Dhirgapatra
- Supuspa
- Chitrapatrika
TYPES
According to Abhidhana ratnamala
- Two varieties
- Mahadrona
- Dronapushpa
According to Raja narahari
- Drona – Lucas aspera
- Mahadrona – L. Cephalotus
- Another species – L. indica
PART USED
- Panchanga
FORMULATION
- Plihari vati
- Gorocanadi vati
- Nimbadilepa
- Sahacharadi taila
DOSAGE
- Swarasa-5-10ml.
- Churna-1-3gm
PROPERTIES
Rasa: katu, lavana, Madhura.
Guna: Guru, Ruksha, Theekshna
Veerya: Ushna.
Vipaka: Madhura
Doshsgnhtha: Kapha, vata, shamaka.
CHEMICAL COMPOSITION
- Its Panchanga contains B-sisstesterol, flavinol, Glycoside.
- Flowers contain an essential oil, A bitter principle seeds a contain a fixed oil , caryophyllene, oxide, 26.56% Gama- Fenchene 12.02%, Alpha- cordional 2.13% , 1-hepten 3-01, 6.53%, menthol 6.30%, deca hydro naphthalene 5.15%, and trans –caryophyllene 4.05%.
- Labdane, Noraladane, laballenic acid lauric acid, glutaric acid, Adipic acid , tridecanoic acid.
KARMA
- Bhedana
- Kaphagna
- Amapacaka
- Kamalahara
- Shothoghna
- Shvasagna
- Krimigana
- Swedajanana
- Vata prashamana
- Samsrana
- Vishamajvarahara
PRAYOGA
- Kaamala
- Shotha
- Shwasa
- Vishamajvara
- Kandu
- Udara shoola
- Pratisyaya
- Jvara
- Shira shoola
THERAPEUTIC USES
Vishamajvara– Fresh juice of dronapuspi and tulasi are useful. [Sharangadhara Samhita madhyamakhanda]
Kaamala: Anjana with the juice of dronapuspi useful. [Gadanigraha].
Netrarogani: dronapuspi juice is mixed with rice water and used orally as well as topically. [G.N]
Pittajavikara : Hima prepared by sariva, rasani, guduchi, rakthachandana and dronapuspi. [Siddhayogasangraha]
Paandu : Hima prepared by dronapuspi and padmaka, sariva drugs are useful. [Siddhayogasangraha]
PHARMACO THERAPEUTIC ACTION AND USES
Lecus cephalotes has been reported to exert hepatoprotective action in carbon tetra chloride induced hepatotoxicity in animals.
Juice of it has been reported to act as an antibilious in herbal therapy for jaundice
It has shown positive test in filariesis
The whole plant powder in the proportion of 70% in the herbal composition is patented to cure epileptic convulsions and cerebral function disorders.
It is also having the properties of antipyretic, stimulant , expectorant, aperients , diaphoretic, insecticidal, emmenagogue, and antioxidant, anti-inflammatory and anti diabetic.
They are useful in colic, dyspepsia arthralgia.
FOLKLORE USES
- Plant decoction is used in the treatment of malarial fever .
- The leaves juice is used topically in psoriasis, skin eruption , and scabies and internally for the treatment of urinary complaints.
- The flowers are administered in the form of syrup or with honey for cough and cold.
- The dried inflorescences are smoked and the smoke exhaled through the nose to treat nose bleeds.
- Dried leaves along with tobacco (1:3) are smoked to treat bleeding as well as itching piles and fresh leaves eaten as a potent herb.
CULTIVATION
Cultivated fields as a weed , especially after a period of rain . It is collected for use as a leafy vegetable in rural areas . it is cultivated itself for its medicinal uses . And really available in market.
RESEARCH STUDIES
ANTIBACTERIAL
Leucas cephalotes a common ethanomedicinal plant’s used by folklore of tirupathi andrapradesh for fever and urinary tract infection. Organic extracts hexane and methanolic extracts showed prominent antibacterial activity .
IN VITRO ANTHELMINTIC ACTIVITY
It is mild stimulant diaphoretic and used for fever
The overall study showed that dronapushpi decoction was beneficial to naveen (new) amavata.
The claim of folk ore amavata probably more beneficial if used with suitable vedanasthapana (analgesic) drugs
Traditional medicinal uses
Dronapushpi is a weed that grows on wastelands. Medicinally, it has antimicrobial, insecticidal, fever reducing, larvicidal and inflammation reducing properties. It is useful in skin diseases. In malarial fever, the leaves juice is given. In some part of country, the decoction of whole plant is used for curing fever. The juice removes toxins from body. The leaves juice is applied externally for skin diseases and swelling. In cod and cough, the leaves juice is recommended.
Scorpion sting
In scorpion sting the plant is used internally as well externally. The leaves juice (few drops) is mixed with honey and taken orally.
Topically, the leaves juice is applied on place of sting.
Snake bite
The folk remedy is to put few drops of whole plant in nostrils.
Skin diseases, removing blood toxins
Skin diseases mainly occur due to toxins in blood. Dronapushpi plant has ability to flush the toxins from body.
In skin diseases, whole plant of Dronapushpi is used. The plant is dried. Five grams of dried powder is taken with three grams Neem/Margosa leaves in 2 glass water. This is boiled till volume reduce to one fourth. Then it filtered and taken two times a day.
Abnormally heavy bleeding at menstruation
The leaves of plant are taken a handful. These are washed and then ground to make fine paste. This paste is mixed with lemon juice and sesame oil/til oil (edible). The preparation is eaten empty stomach every morning for a week.
Asthma, cold, cough
The leaves juice of plant is taken in dose of 1-3 teaspoons.
Excessive thirst
The flowers (2 tablespoon) are boiled in water (150 ml) till volume reduces to half. This is filtered and taken thrice a day.
Cough, leucorrhoea
The leaves of plant are cooked and eaten with rice.
Skin diseases (itching, patchy skin, psoriasis, scabies etc.)
The paste of leaves is applied externally at the affected body areas.
Cough, congestion, blockage of nose, headache due to cough, Sinusitis, Migraine, Phlegm
The juice of leaves is put in nostrils as drops. For this purpose, the leaves juice is extracted and mixed with two times water. Then the diluted juice is put in nostrils (4 dops) for 3-4 days.
The flowers are heated in til/sesame oil and applied on head.
Fever (acute, chronic), Allergy
The decoction of plant (2-3 grams in boiled in two glass water till water reduces to one fourth) is used
This medicinal herb should be used in recommended doses only. It is hot in potency and heats up body. Avoid its use in excess. The leaves juice can be diluted for putting in nose of oral use.
………..
SHIMOGA, KARNATAKA, INDIA
Shimoga – Wikipedia, the free encyclopedia
Shimoga, officially renamed as Shivamogga, is a city and the district headquarters of Shimoga District in the central part of the state of Karnataka, India. The city …
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Shimoga–Talaguppa railway
Kundadri, Shimoga
Shimoga Photos – Kudli Temple
Ornate baluster in Thripuranthakeshwara temple at Balligavi, Shimoga district.jpg
sigandur – Shimoga
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New Drug Approvals 