Abstract:
:Canagliflozin (Invokana™), an oral selective sodium-glucose co-transporter 2 (SGLT2) inhibitor, is under global development with Mitsubishi Tanabe Pharma and Janssen Pharmaceuticals, a subsidiary of Johnson and Johnson, for the treatment of type 2 diabetes mellitus. SGLT2 are mainly located in the proximal tubule of the kidney and are involved in the reabsorption of filtered glucose from the glomeruli into the body. Inhibition of SGLT2 lowers blood glucose in an insulin independent manner as a consequence of blocking reabsorption of filtered glucose in the glomeruli, thereby increasing urinary excretion of glucose and, in turn, potentially reducing bodyweight. Canagliflozin is the first SGLT2 inhibitor to be approved in the USA and is under regulatory review in the EU. This article summarizes the milestones in the development of canagliflozin, leading to its first approval for use in adults with type 2 diabetes.
journal_name
Drugsjournal_title
Drugsauthors
Elkinson S,Scott LJdoi
10.1007/s40265-013-0064-9subject
Has Abstractpub_date
2013-06-01 00:00:00pages
979-88issue
9eissn
0012-6667issn
1179-1950journal_volume
73pub_type
杂志文章,评审相关文献
DRUGS文献大全abstract::Trigeminal neuralgia is a representative neuropathic facial pain condition, characterised by unilateral paroxysmal pain in the distribution territory of one or more divisions of the trigeminal nerve, triggered by innocuous stimuli. A subgroup of patients with trigeminal neuralgia [TN (previously defined as atypical TN...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-018-0964-9
更新日期:2018-09-01 00:00:00
abstract::Fluticasone furoate nasal spray is a new topical intranasal corticosteroid with enhanced affinity for the glucocorticoid receptor and low systemic exposure, which was recently approved in the US for the treatment of seasonal or perennial allergic rhinitis in adults and in children aged >or=2 years. Fluticasone furoate...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200767130-00010
更新日期:2007-01-01 00:00:00
abstract::Pain is an unpleasant sensation that originates from ongoing or impending tissue damage. Management of different types of pain (acute, postoperative, inflammatory, neuropathic or cancer) is the most frequent issue encountered by clinicians and pharmacological therapy is the first line of approach for the treatment of ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200767150-00002
更新日期:2007-01-01 00:00:00
abstract::The role of serotonin in the pathogenesis of hypertension is not clear. Serotonin is produced by the enterochromaffin cells of the gut; the greater part of this is metabolised in the liver and lungs and nearly all of the remainder is taken up by the platelets. Consequently, circulating levels of serotonin are extremel...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/00003495-198800361-00011
更新日期:1988-01-01 00:00:00
abstract::Drug-resistant tuberculosis (DR-TB) is an emerging global health threat as treatment involves complex multiple drug regimens, which are longer and more toxic than standard therapy and yet have worse outcomes. In the presence of resistance to one or more first-line drugs, an alternative regimen should be designed. A ma...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/11585440-000000000-00000
更新日期:2011-05-07 00:00:00
abstract::Mortality and morbidity in gastroenteritis in children is the result of fluid loss, acid-base and electrolyte imbalance. Hence therapy should be aimed at preventing or correcting this imbalance. The use of intestinal antibiotics to treat the condition should not be a routine, but parenteral antibiotic therapy in the p...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-197611040-00004
更新日期:1976-01-01 00:00:00
abstract::Pruritus is a common complication of end-stage renal disease (ESRD), affecting about one-third of dialysis patients. It is a chronic, unpleasant symptom with a strong negative impact on patients' quality of life, often inducing sleeplessness and mood disorders. Recent data show that it is also associated with increase...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200969030-00002
更新日期:2009-01-01 00:00:00
abstract::Peripheral arterial occlusive disease is a common condition with possible serious consequences. It is usually diagnosed at the intermittent claudication stage. There are 2 objectives of treatment: to prevent ischaemic attacks and to improve quality of life. Treatment efficacy is, however, usually evaluated only in ter...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199856003-00004
更新日期:1998-01-01 00:00:00
abstract::The benefits of the treatment of hypertension currently consist of a substantially reduced incidence of premature stroke, left ventricular failure and malignant hypertension. The benefits for the individual are most clearcut in those who have already had severe or symptomatic hypertension. Older subjects who have a hi...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198800366-00003
更新日期:1988-01-01 00:00:00
abstract:UNLABELLED:Joint pain is the main complaint in patients affected by osteoarthritis (OA), and NSAIDs are commonly used to treat pain associated with OA. Over the past few years, cyclo-oxygenase (COX)-2-selective inhibitors have been proved to have certain advantages over non-selective NSAIDs and have been increasingly u...
journal_title:Drugs
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003495-200363001-00006
更新日期:2003-01-01 00:00:00
abstract::Levetiracetam (Keppra®, E Keppra®) is an established second-generation antiepileptic drug (AED). Worldwide, levetiracetam is most commonly approved as adjunctive treatment of partial onset seizures with or without secondary generalization; other approved indications include monotherapy treatment of partial onset seizu...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/11204490-000000000-00000
更新日期:2011-03-05 00:00:00
abstract::Alteplase is the product of recombinant DNA technology and is chemically identical to endogenous tissue-type plasminogen activator: Plasminogen is converted to plasmin by alteplase, and fibrinolysis of blood thrombi is subsequently stimulated. Alteplase is now firmly established as a treatment of choice in the managem...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199550020-00007
更新日期:1995-08-01 00:00:00
abstract::The efficacy and safety of rectally administered nimesulide 200mg and paracetamol 500mg were assessed in a double-blind study. The study was conducted in 39 elderly inpatients with infections of the upper or lower respiratory tract associated with fever; 18 patients received nimesulide and 21 received paracetamol. Bot...
journal_title:Drugs
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003495-199300461-00026
更新日期:1993-01-01 00:00:00
abstract::Glatiramer acetate is a synthetic analogue of the multiple sclerosis (MS)-associated antigen, myelin basic protein. It is indicated in the EU, US and many other countries to reduce the frequency of relapses in patients with relapsing-remitting MS (RRMS), and for the treatment of patients who have experienced a well de...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/11204560-000000000-00000
更新日期:2010-08-20 00:00:00
abstract::Acyclovir (aciclovir) is a nucleoside antiviral drug with antiviral activity in vitro against members of the herpes group of DNA viruses. As an established treatment of herpes simplex infection, intravenous, oral and to a lesser extent topical formulations of acyclovir provide significant therapeutic benefit in genita...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198937030-00002
更新日期:1989-03-01 00:00:00
abstract::Eltrombopag (Revolade(®)) is an orally bioavailable, low molecular weight, synthetic nonpeptide thrombopoietin receptor agonist, which selectively binds to the transmembrane and juxtamembrane domains of the thrombopoietin receptor on the surface of platelets, megakaryocytes and megakaryocyte precursor cells, resulting...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/11207390-000000000-00000
更新日期:2011-07-09 00:00:00
abstract::Rapid progress has recently been encountered in pharmacologically treating the unborn baby. This unique area of drug therapy raises new methodological and ethical questions. This article is a systematic review of known modalities of fetal pharmacotherapy, and aims to highlight essential principles, difficulties and co...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200262050-00004
更新日期:2002-01-01 00:00:00
abstract::A somatropin preparation (Zorbtive) produced by recombinant DNA technology has been evaluated in patients with short bowel syndrome. Somatropin is thought to enhance intestinal adaptation in this condition through direct or indirect effects on the intestine. In a randomised, double-blind study in patients with short b...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200464120-00008
更新日期:2004-01-01 00:00:00
abstract::The incidence of pulmonary embolism (PE) and venous thromboembolism (VTE) is higher in pregnant patients than in non-pregnant patients. The incidence of thrombosis in all pregnancies is reported to be between 0.05 and 1%, and an incidence as high as 3% may be present in women after caesarean section. Anticoagulant med...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200262030-00004
更新日期:2002-01-01 00:00:00
abstract::Alfuzosin, a new quinazoline derivative, acts as a selective and competitive antagonist of alpha 1-adrenoceptor-mediated contraction of prostatic, prostatic capsule, bladder base and proximal urethral smooth muscle, thereby reducing the tone of these structures. Consequently, urethral pressure and resistance, bladder ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199345030-00008
更新日期:1993-03-01 00:00:00
abstract::The 'funny' (pacemaker, I(f)) current, first described almost 30 years ago in sinoatrial node (SAN) myocytes, is a mixed sodium/potassium inward current, activated on hyperpolarisation in the diastolic range of voltages. 'Funny' (f) channels are activated by intracellular cyclic adenosine monophosphate (cAMP) concentr...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200767002-00003
更新日期:2007-01-01 00:00:00
abstract::Lung function can be reduced not only by a non-selective beta-blocker but also by a selective beta1-receptor blocker. If both types of drug are without intrinsic sympathomimetic activity, the effect of the non-selective drug is more pronounced than that of a beta1-receptor selective drug under basal conditions. The ef...
journal_title:Drugs
pub_type: 临床试验,杂志文章
doi:10.2165/00003495-197600111-00035
更新日期:1976-01-01 00:00:00
abstract::The article Trifluridine/Tipiracil: A Review in Metastatic Gastric Cancer, written by Connie Kang, Sohita Dhillon and Emma D. Deeks, was originally published Online First without open access. ...
journal_title:Drugs
pub_type: 杂志文章,已发布勘误
doi:10.1007/s40265-019-01199-6
更新日期:2019-10-01 00:00:00
abstract::Specifically formulated for nebulisation using the PARI LC PLUS reusable nebuliser, tobramycin solution for inhalation (TSI) [TOBI] provides a high dose of tobramycin (an aminoglycoside antibacterial with good activity against Pseudomonas aeruginosa) to the lungs of patients with cystic fibrosis, while maintaining low...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200363220-00015
更新日期:2003-01-01 00:00:00
abstract::Nateglinide is a novel D-phenylalanine derivative that inhibits ATP-sensitive K+ channels in pancreatic beta-cells in the presence of glucose and thereby stimulates the prandial release of insulin. Nateglinide reduces fasting and mealtime blood glucose levels in animals, healthy volunteers, and patients with type 2 (n...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200060030-00007
更新日期:2000-09-01 00:00:00
abstract::All male inhabitants of the city of Göteborg, who were born between 1915-1922 and 1924-1925 were included in the trial, and were 47 to 55 years of age on entry to the study in 1970 to 1973. One-third of these men were randomly allocated to an intervention group, whilst the other two-thirds acted as controls. Men of al...
journal_title:Drugs
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003495-198600311-00009
更新日期:1986-01-01 00:00:00
abstract::Available data indicate that the most common beta-lactamase produced by Branhamella catarrhalis is plasmid mediated. The same enzyme occurs in Moraxella nonliquefaciens, a commensal in the upper respiratory tract. The ability to produce the enzyme, which is known as BRO-1, can be transferred by conjugation from M. non...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/00003495-198600313-00026
更新日期:1986-01-01 00:00:00
abstract::Anthracyclines are among the most active drugs for the treatment of advanced breast cancer. Epirubicin has been found to be as effective as doxorubicin at equimolar doses but significantly better tolerated, especially in terms of alopecia, leucopenia, and cardiac toxicity. The role of anthracycline-containing regimens...
journal_title:Drugs
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003495-199300452-00007
更新日期:1993-01-01 00:00:00
abstract::This paper reviews the theoretical concepts and methods utilised with isolated tissues to characterise drugs and drug receptors. Specifically the impact, on the in vitro measurement of agonist affinity and relative efficacy, of the idea that receptors bind to transduction proteins in the lipid bilayer of the cell memb...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199040050-00003
更新日期:1990-11-01 00:00:00
abstract::Scleroderma or systemic sclerosis is a rare condition with many clinical manifestations including Raynaud's phenomenon. As with many other rarely encountered diseases, drug therapy for scleroderma is often empirical with little evidence in the form of randomised controlled trials to aid drug choice. Raynaud's phenomen...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200161030-00008
更新日期:2001-01-01 00:00:00