Abstract:
:Avapritinib (AYVAKIT™) is a potent and selective tyrosine kinase inhibitor of platelet-derived growth factor receptor alpha (PDGFRA) and KIT activation loop mutants. It is being developed by Blueprint Medicines for the treatment of gastrointestinal stromal tumours (GIST), solid tumours and systemic mastocytosis. Avapritinib is approved in the USA for PDGFRA exon 18 (including D842V) mutant GIST and is undergoing regulatory assessment in the USA as a 4th-line treatment for GIST. Avapritinib is also undergoing regulatory assessment in the EU for PDGFRA D842V mutant GIST. This article summarizes the milestones in the development of avapritinib leading to this first approval for the treatment of adults with unresectable or metastatic GIST harbouring a PDGFRA exon 18 mutation, including PDGFRA D842V mutations. Clinical development of avapritinib is also underway for the treatment of systemic mastocytosis and late-stage solid tumours in several countries.
journal_name
Drugsjournal_title
Drugsauthors
Dhillon Sdoi
10.1007/s40265-020-01275-2subject
Has Abstractpub_date
2020-03-01 00:00:00pages
433-439issue
4eissn
0012-6667issn
1179-1950pii
10.1007/s40265-020-01275-2journal_volume
80pub_type
杂志文章,评审相关文献
DRUGS文献大全abstract::Tuberculosis continues to be a major cause of disease and death throughout the developing world. Chemotherapy is the current method of control but with the continuing emergence of drug resistance, coupled with the reticence of major drug companies to invest in drug discovery, the identification of new vaccines to comb...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/00003495-200565170-00002
更新日期:2005-01-01 00:00:00
abstract::Echinocandins are a new class of antifungal agents with a novel mechanism of action (interference with fungal cell wall synthesis). Caspofungin (Cancidas), Caspofungin MSD) is the first echinocandin to be approved and is administered intravenously. Caspofungin 50 mg/day had similar efficacy to intravenous fluconazole ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200363200-00008
更新日期:2003-01-01 00:00:00
abstract::Stroke is the third most common cause of death in the US. Primary prevention of stroke can be achieved by control of risk factors including hypertension, diabetes mellitus, elevated cholesterol levels and smoking. Approximately one-third of all ischaemic strokes occur in patients with a history of stroke or transient ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200565040-00003
更新日期:2005-01-01 00:00:00
abstract::Amiodarone is a class III antiarrhythmic drug with sympatholytic properties, which prolongs the refractory period of all cardiac tissues, depresses sinus node automaticity and atrioventricular nodal conduction. It is active on all cardiac arrhythmias, its use being limited by the risk of side effects, mainly extracard...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199100412-00009
更新日期:1991-01-01 00:00:00
abstract::Interstitial lung disease (ILD) can be associated with all connective tissue diseases and is an important cause of morbidity and mortality. The management of connective tissue disease-interstitial lung disease (CTD-ILD) is challenging due substantial heterogeneity in disease behaviour and paucity of controlled clinica...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-019-01178-x
更新日期:2019-09-01 00:00:00
abstract::The emergence of antibiotic resistance is primarily due to excessive and often unnecessary use of antibiotics in humans and animals. Risk factors for the spread of resistant bacteria in hospitals and the community can be summarised as over-crowding, lapses in hygiene or poor infection control practices. Increasing ant...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199855030-00001
更新日期:1998-03-01 00:00:00
abstract::Information about the value for money of a medicine as derived from an economic evaluation can be used for decision-making purposes by policy makers, healthcare payers, healthcare professionals and pharmaceutical companies. This article illustrates the use of economic evaluation by decision makers and formulates a num...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/11538120-000000000-00000
更新日期:2010-10-22 00:00:00
abstract::The cardinal haemodynamic disturbance in established hypertension is an increased total peripheral resistance and a subnormal blood flow, particularly during exercise. The spontaneously occurring changes in central haemodynamics have been followed in young males with essential hypertension over a 17-year period: a gra...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198400282-00004
更新日期:1984-01-01 00:00:00
abstract:UNLABELLED:5-Methoxypsoralen, a naturally occurring linear furocoumarin, has been successfully used in combination with ultraviolet (UV) A irradiation [psoralen plus UV (PUVA)] to manage psoriasis and vitiligo. In patients and volunteers, PUVA 5-methoxypsoralen causes a dose-related increase in cutaneous photosensitivi...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199856040-00015
更新日期:1998-10-01 00:00:00
abstract::Potassium channel openers or agonists represent a novel new class of compounds in the treatment of a range of cardiovascular disorders, particularly angina pectoris and hypertension. Nicorandil is the only clinically available potassium channel opener with antianginal effects, and with comparable efficacy and tolerabi...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200161120-00002
更新日期:2001-01-01 00:00:00
abstract::Capecitabine is an orally administered fluoropyrimidine carbamate used for the treatment of paclitaxel- or anthracycline-refractory breast cancer. Capecitabine is metabolised via a 3-step process to the active agent fluorouracil. The final step of this process occurs preferentially in malignant tissue. In patients wit...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199958010-00006
更新日期:1999-07-01 00:00:00
abstract::Crizotinib (Xalkori(®)) is an orally active, small molecule inhibitor of multiple receptor tyrosine kinases, including anaplastic lymphoma kinase (ALK), c-Met/hepatocyte growth factor receptor and c-ros oncogene 1. In the EU, crizotinib has been conditionally approved for the treatment of adults with previously treate...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-013-0142-z
更新日期:2013-12-01 00:00:00
abstract::Pomalidomide (Imnovid®; Pomalyst®), an analogue of thalidomide, is an immunomodulatory agent, with several mechanisms of action (both direct and indirect) thought to be involved in its anti-myeloma activity. Oral pomalidomide is available in several countries for use in combination with low-dose dexamethasone in adult...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-017-0833-y
更新日期:2017-11-01 00:00:00
abstract::Hirsuties and androgenic alopecia are the patterns of hair growth in women which develop in a similar manner to that normally seen in men. This process is mediated by androgens. It may be due to increased hormone production or increased target organ sensitivity. The majority of patients with hirsuties may be adequatel...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198835010-00005
更新日期:1988-01-01 00:00:00
abstract::Buflomedil hydrochloride is a vasoactive drug with a variety of pharmacodynamic properties. Importantly, it seems to improve nutritional blood flow in ischaemic tissue of patients with peripheral and/or cerebral vascular disease by a combination of pharmacological effects: inhibition of alpha-adrenoceptors, inhibition...
journal_title:Drugs
pub_type: 临床试验,杂志文章,评审
doi:10.2165/00003495-198733050-00002
更新日期:1987-05-01 00:00:00
abstract::Inhaled mometasone furoate (Asmanex) is a synthetic corticosteroid indicated for the first-line maintenance prophylactic therapy of persistent asthma in adults and adolescents. It is formulated for delivery via a breath-actuated dry powder inhaler (DPI) [Twisthaler].Inhaled mometasone furoate delivered by DPI is effec...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200666080-00011
更新日期:2006-01-01 00:00:00
abstract::Tenoxicam is a new non-steroidal anti-inflammatory and analgesic agent of the oxicam class, and therefore closely related to piroxicam. It possesses a long half-life which enables it to be administered once daily. Clinical trials in patients with rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout and n...
journal_title:Drugs
pub_type: 临床试验,杂志文章,评审
doi:10.2165/00003495-198734030-00001
更新日期:1987-09-01 00:00:00
abstract::Hepatitis E accounts for the major part of enterally transmitted non-A, non-B hepatitis worldwide. Its agent, the hepatitis E virus (HEV), is a small, single-stranded RNA virus. Only one serotype of HEV is recognised. Infection results in protective immunity with long-lived neutralising antibodies. In developing count...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200464140-00002
更新日期:2004-01-01 00:00:00
abstract::Empagliflozin/linagliptin (Glyxambi(®)) is a once-daily sodium glucose co-transporter type 2 (SGLT2) inhibitor and dipeptidyl peptidase (DPP)-4 inhibitor fixed-dose combination product that is approved in the USA as an adjunct to diet and exercise in adults with type 2 diabetes (T2D) when treatment with both empaglifl...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-015-0457-z
更新日期:2015-09-01 00:00:00
abstract::The size of the antibiotic market in developing countries is double that seen in developed countries. There are some valid reasons for this difference, one of which is the higher frequency of diverse infections in the developing world. However, other factors are involved: for example, antibiotics are available without...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199300453-00009
更新日期:1993-01-01 00:00:00
abstract::Schistosomiasis, a grave and debilitating disease of socioeconomic importance, is increasing in incidence despite concerted efforts to control and contain the disease in all the endemic areas. While a multipronged method of control using health education, sanitation and snail control has been used, chemotherapy and ch...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199142030-00004
更新日期:1991-09-01 00:00:00
abstract::Platinum-based doublet chemotherapy with or without bevacizumab is the standard of care for the initial management of advanced and metastatic non-small cell lung cancer (NSCLC) without a targetable molecular abnormality. However, the majority of patients with NSCLC will ultimately develop resistance to initial platinu...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-016-0628-6
更新日期:2016-09-01 00:00:00
abstract::Miconazole is an imidazole antifungal drug which has recently become available for systemic use. Its antifungal activity has been well studied and it is active in vitro against a wide range of fungi. Published and unpublished reports of the use of miconazole in conditions such as systemic or mucocutaneous candidosis, ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198019010-00002
更新日期:1980-01-01 00:00:00
abstract::204 individuals from a rural community were given a single dose of oxantel-pyrantel at 15mg/kg bodyweight and if still infected, 20mg/kg bodyweight, with cure rates of 100%, 53% and 71% for ascariasis, trichuriasis and hookworm infection, respectively. From an urban community, 124 patients were given the same drug eit...
journal_title:Drugs
pub_type: 临床试验,杂志文章
doi:10.2165/00003495-197800151-00016
更新日期:1978-01-01 00:00:00
abstract::The sensitivity to cefotaxime and amikacin of 14,272 Gram-negative bacilli (Enterobacteriaceae and non-fermenting Gram-negative bacilli) isolated from clinical samples was studied during the period 1980 to 1985. The minimum inhibitory concentration (MIC) was determined by means of diffusion in agar. Strains were consi...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/00003495-198800352-00003
更新日期:1988-01-01 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::Nizatidine is an H2-receptor antagonist which in animal studies was more active on a weight-for-weight basis than cimetidine in inhibiting basal and stimulated gastric acid secretion. Similarly, studies in humans have confirmed that nizatidine is a potent inhibitor of basal, nocturnal and stimulated gastric acid secre...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198836050-00002
更新日期:1988-11-01 00:00:00
abstract::Onychomycoses, infections of the nail caused by fungi, are amongst the most common illnesses. Because of the high incidence of these infections and problems involved in their therapy, they have received much attention, particularly as concerns a better characterisation of the causative micro-organisms. Onychomycosis c...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199958020-00005
更新日期:1999-08-01 00:00:00
abstract:UNLABELLED:Ofloxacin is an established fluoroquinolone agent which achieves good concentrations in genitourinary tract tissues and fluids. It has good in vitro activity against most Enterobacteriaceae, Staphylococcus saprophyticus, methicillin-susceptible S. aureus, Neisseria gonorrhoeae, Chlamydia trachomatis and Haem...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199856050-00015
更新日期:1998-11-01 00:00:00
abstract::The management of mediastinitis involves directing appropriate antibacterial therapy against the potential bacterial pathogens. The increased recovery of anaerobic bacteria from mediastinal infections has led to a greater appreciation of their role in this condition and to re-evaluation of the proper treatment of this...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200666030-00004
更新日期:2006-01-01 00:00:00