Lack of Susceptibility of Bicyclic Nucleoside Analogs, Highly Potent
... dihydropyrimidine dehydrogenase (DPD), the key catabolic enzyme in the degradation of pyrimidine nucleosides (Desgranges et al., 1986). The latter property underlies the severe toxicity that led to a number of deaths of persons who were exposed to the anticancer drug 5-fluorouracil (FU) in combinati ...
... dihydropyrimidine dehydrogenase (DPD), the key catabolic enzyme in the degradation of pyrimidine nucleosides (Desgranges et al., 1986). The latter property underlies the severe toxicity that led to a number of deaths of persons who were exposed to the anticancer drug 5-fluorouracil (FU) in combinati ...
Inhaled phosphodiesterase type 5 inhibitors restore chloride transport in cystic fibrosis mice
... delivered orally [2]. Nebulisation of topically active drugs has become increasingly common for treatment in CF [3]. Novel drug formulations acting through distinct mechanisms, including restoration of airway surface liquid or mucus, anti-inflammatory or anti-infective agents, and immunosuppressive ...
... delivered orally [2]. Nebulisation of topically active drugs has become increasingly common for treatment in CF [3]. Novel drug formulations acting through distinct mechanisms, including restoration of airway surface liquid or mucus, anti-inflammatory or anti-infective agents, and immunosuppressive ...
Fragment-Based Discovery of the Pyrazol-4
... known to be important regulators of mitosis.14 In recent years, two isoforms, Aurora A and Aurora B, have been of considerable interest as targets in the discovery of new anticancer drugs.15 This interest stems from the fact that both isoforms are found overexpressed in solid tumors and leukemias.16 ...
... known to be important regulators of mitosis.14 In recent years, two isoforms, Aurora A and Aurora B, have been of considerable interest as targets in the discovery of new anticancer drugs.15 This interest stems from the fact that both isoforms are found overexpressed in solid tumors and leukemias.16 ...
Aripiprazole LAI Prescribing Guidelines
... gluteal muscle (no sooner than 26 days after the previous injection). 6. Oral aripiprazole at 10mg-20mg per day must continue for two weeks after the first injection to maintain therapeutic aripiprazole concentrations during initiation of therapy. 7. As aripiprazole LAI requires oral supplementation ...
... gluteal muscle (no sooner than 26 days after the previous injection). 6. Oral aripiprazole at 10mg-20mg per day must continue for two weeks after the first injection to maintain therapeutic aripiprazole concentrations during initiation of therapy. 7. As aripiprazole LAI requires oral supplementation ...
A Novel Model for the Prediction of Drug
... concentration, the portal vein concentration, the steady-state systemic plasma concentration, a multiple (such as 10⫻) of the plasma concentration, the maximum plasma concentration, the maximum hepatic input concentration, or the liver concentration (Blanchard et al., 2004; Cook et al., 2004; Ito et ...
... concentration, the portal vein concentration, the steady-state systemic plasma concentration, a multiple (such as 10⫻) of the plasma concentration, the maximum plasma concentration, the maximum hepatic input concentration, or the liver concentration (Blanchard et al., 2004; Cook et al., 2004; Ito et ...
Identification of GZD824 as an Orally Bioavailable Inhibitor That
... and AblY253F, respectively; thus, this compound was 40−120fold less potent than 10a. The removal of a hydrogen bond donor in the hinge-binding region (23b and 24) also induced an obvious loss of potency. A minor structural modification was also introduced to investigate the potential impact of R1 and ...
... and AblY253F, respectively; thus, this compound was 40−120fold less potent than 10a. The removal of a hydrogen bond donor in the hinge-binding region (23b and 24) also induced an obvious loss of potency. A minor structural modification was also introduced to investigate the potential impact of R1 and ...
... activity, is an antagonist at adenosine receptors, blockade of adenosine activity has been proposed as a possible mechanism for theophylline's effects in asthma [30]. In human bronchial smooth muscle, however, 8-phenyltheophylline - a methylxanthine adenosine antagonist with negligible PDE inhibitor ...
Beware: Clinically Significant Drug Interactions in the Treatment of HIV
... Mechanism of ARV Drug Interactions • Most clinically relevant antiretroviral (ARV) drug ...
... Mechanism of ARV Drug Interactions • Most clinically relevant antiretroviral (ARV) drug ...
The Safety of COX
... A proposal by Merck to reintroduce Vioxx to the market would require a supplemental new drug application. Such an application would be reviewed with consideration of the risk to benefit balance of the proposed indications and populations for use, warnings in the label, and all relevant data. We expe ...
... A proposal by Merck to reintroduce Vioxx to the market would require a supplemental new drug application. Such an application would be reviewed with consideration of the risk to benefit balance of the proposed indications and populations for use, warnings in the label, and all relevant data. We expe ...
Hit discovery and hit-to-lead approaches
... suitable high-throughput assay can be developed for HTS. Novel ideas generated by information on small molecules reported in the literature are potentially the fastest entry to new leads for validated targets. In addition, in silico methods remain an attractive option for prioritizing structures for ...
... suitable high-throughput assay can be developed for HTS. Novel ideas generated by information on small molecules reported in the literature are potentially the fastest entry to new leads for validated targets. In addition, in silico methods remain an attractive option for prioritizing structures for ...
REVIEWS
... The therapeutic value of targeting members of the CDK family has been intensively studied, particularly for interphase CDKs (CDK2, CDK4 and CDK5); CDK1 is also emerging as a potential new target. other CDKs that are not involved in the cell cycle have specific functions in particular processes or ce ...
... The therapeutic value of targeting members of the CDK family has been intensively studied, particularly for interphase CDKs (CDK2, CDK4 and CDK5); CDK1 is also emerging as a potential new target. other CDKs that are not involved in the cell cycle have specific functions in particular processes or ce ...
Syddansk Universitet The Monoamine Oxidase Inhibitor
... The early MAOI diets recommended were unnecessarily restrictive. In fact, very few foods have sufficient tyramine content to approach the threshold of a serious hypertensive reaction [28]. A high-tyramine meal, however, is sufficient to increase blood pressure critically, when a substantial part of ...
... The early MAOI diets recommended were unnecessarily restrictive. In fact, very few foods have sufficient tyramine content to approach the threshold of a serious hypertensive reaction [28]. A high-tyramine meal, however, is sufficient to increase blood pressure critically, when a substantial part of ...
Drug-Drug Interactions Among Hepatitis C Virus (HCV) and Human
... in this patient population is critical, as coinfection has been linked to deterioration of both disease states. The objective of this review article is to highlight the current literature on drug-drug interactions between HIV and HCV treatments. The management of the treatment of coinfection patient ...
... in this patient population is critical, as coinfection has been linked to deterioration of both disease states. The objective of this review article is to highlight the current literature on drug-drug interactions between HIV and HCV treatments. The management of the treatment of coinfection patient ...
Interactive Properties of Tizanidine (Zanaflex)
... healthy subjects, pretreatment with fluvoxamine (100 mg/day for 4 days) resulted in a dramatic 33-fold increase in tizanidine area under the plasma concentration–time curve (AUC).1 The marked increases in tizanidine plasma concentrations were accompanied by pharmacodynamic changes, such as marked re ...
... healthy subjects, pretreatment with fluvoxamine (100 mg/day for 4 days) resulted in a dramatic 33-fold increase in tizanidine area under the plasma concentration–time curve (AUC).1 The marked increases in tizanidine plasma concentrations were accompanied by pharmacodynamic changes, such as marked re ...
Synopsis of Some Recent Tactical Application of Bioisosteres in
... context of inhibitors of kinesin spindle protein (KSP), a family of motor proteins that represents a novel mechanistic target for the treatment of taxane-refractory solid tumors.57 Optimization of a dihydropyrrole-based series of KSP inhibitors identified 22 as an advanced molecule in which the CH2O ...
... context of inhibitors of kinesin spindle protein (KSP), a family of motor proteins that represents a novel mechanistic target for the treatment of taxane-refractory solid tumors.57 Optimization of a dihydropyrrole-based series of KSP inhibitors identified 22 as an advanced molecule in which the CH2O ...
Oral Therapies for Cancer - Oncology Nursing Society
... early breast cancer, as first line therapy for postmenopausal women with hormone receptor positive or hormone receptor unknown locally advanced or metastatic breast cancer, and for treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy. ...
... early breast cancer, as first line therapy for postmenopausal women with hormone receptor positive or hormone receptor unknown locally advanced or metastatic breast cancer, and for treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy. ...
Anticonvulsants - LSU School of Medicine
... • Simple Partial: Person may experience a range of strange or unusual sensations. ...
... • Simple Partial: Person may experience a range of strange or unusual sensations. ...
Drugs acting on RAAS by Dr Vignesh S
... bradykinin and other ACE substrates ◦ No rise in level or potentiation of bradykinin, substance P occurs. ACEI related cough is rare ...
... bradykinin and other ACE substrates ◦ No rise in level or potentiation of bradykinin, substance P occurs. ACEI related cough is rare ...
Pipeline/Commercial Insight: Molecular Targeted Cancer
... stimulator that has reached the market and achieved success in the treatment of multiple myeloma, another product in this class, Genta’s Genasense, has suffered significant setbacks in its commercialization. As evidenced here, although Genasense has been at an advanced stage of development for sever ...
... stimulator that has reached the market and achieved success in the treatment of multiple myeloma, another product in this class, Genta’s Genasense, has suffered significant setbacks in its commercialization. As evidenced here, although Genasense has been at an advanced stage of development for sever ...
IDrugs The Investigational Drugs Journal
... with relief lasting up to one year. Bone marrow toxicity was also much less than comparable therapies. Two multi-center, double-blind, randomized clinical trials are currently in progress in 100 prostate cancer patients and 75 patients with osteolytic bone metastases (including breast and lung). Thi ...
... with relief lasting up to one year. Bone marrow toxicity was also much less than comparable therapies. Two multi-center, double-blind, randomized clinical trials are currently in progress in 100 prostate cancer patients and 75 patients with osteolytic bone metastases (including breast and lung). Thi ...
Pharmacology Objectives 7
... *Loop diuretics are appropriate for edematous disorders in all but emergent situations Hydrochlorothiazide Antihypertension treatment, edema states, Ca+ nephrolithaisis, Osteoporosis, nephrogenic diabetes insipidous Triamterene & Not very efficacious, for use in combination with loop diuretics or Am ...
... *Loop diuretics are appropriate for edematous disorders in all but emergent situations Hydrochlorothiazide Antihypertension treatment, edema states, Ca+ nephrolithaisis, Osteoporosis, nephrogenic diabetes insipidous Triamterene & Not very efficacious, for use in combination with loop diuretics or Am ...
Blood Drugs
... Exert their anticoagulant effect by directly binding to the active site of thrombin, thereby inhibiting thrombin's downstream effects ...
... Exert their anticoagulant effect by directly binding to the active site of thrombin, thereby inhibiting thrombin's downstream effects ...
Doxycycline-coated sutures improve mechanical strength of intestinal anastomoses
... Anastomotic leakage is a major and unresolved problem in patients undergoing colonic or rectal resection [1]. Under experimental conditions, the strength of intestinal anastomoses diminishes postoperatively reaching a minimum on the third postoperative day [2,3]. Increased matrix metalloproteinase ( ...
... Anastomotic leakage is a major and unresolved problem in patients undergoing colonic or rectal resection [1]. Under experimental conditions, the strength of intestinal anastomoses diminishes postoperatively reaching a minimum on the third postoperative day [2,3]. Increased matrix metalloproteinase ( ...
CRIXIVAN - cri.or.th
... utero exposure to ZDV has not demonstrated any tumor development.(93) However, no data is available on longer follow-up for late effects. + These effects seen at only at maternally toxic doses. Nursing Mothers: Studies in lactating rats have demonstrated that indinavir is excreted in milk. Although ...
... utero exposure to ZDV has not demonstrated any tumor development.(93) However, no data is available on longer follow-up for late effects. + These effects seen at only at maternally toxic doses. Nursing Mothers: Studies in lactating rats have demonstrated that indinavir is excreted in milk. Although ...
Selective Inhibitors of Picornavirus Replication
... identified. Most receptors belong to the immunoglobulin (IgSF) superfamily. These molecules consist of tandem repeats of between two and five Ig-like domains.29 Known IgSF receptors for picornaviruses are intercellular adhesion molecule-1 (ICAM-1 or CD54) for major-group rhinoviruses, the poliovirus ...
... identified. Most receptors belong to the immunoglobulin (IgSF) superfamily. These molecules consist of tandem repeats of between two and five Ig-like domains.29 Known IgSF receptors for picornaviruses are intercellular adhesion molecule-1 (ICAM-1 or CD54) for major-group rhinoviruses, the poliovirus ...