![Done By: Sanaa Otoom Advanced Technology Lecture# 2 Last](http://s1.studyres.com/store/data/001362360_1-189bbaf6e43b46c280004cf2dc90e0e5-300x300.png)
Done By: Sanaa Otoom Advanced Technology Lecture# 2 Last
... crystalline form A to crystalline form B or amorphous form” in this case we change the solubility and dissolution accordingly. The same for salts and cocrystals. From slide 15: Pro-drug (?) why question mark? Because prodrug may either increase or decrease the solubility by this approach. Example: ...
... crystalline form A to crystalline form B or amorphous form” in this case we change the solubility and dissolution accordingly. The same for salts and cocrystals. From slide 15: Pro-drug (?) why question mark? Because prodrug may either increase or decrease the solubility by this approach. Example: ...
drugs in Dyslipidaemias
... Bile acid binding resins • Cationic polymer resins that bind non-covalently to negatively-charged bile acids in small intestine • Enterohepatic circulation of bile acids interrupted causing up-regulation of 7αhydroxylase in hepatocytes ...
... Bile acid binding resins • Cationic polymer resins that bind non-covalently to negatively-charged bile acids in small intestine • Enterohepatic circulation of bile acids interrupted causing up-regulation of 7αhydroxylase in hepatocytes ...
Product Information: Dolutegravir (as sodium)
... against 2 non-nucleoside (NN)-RTI-resistant, 3 nucleoside (N)-RTI-resistant, and 2 PIresistant HIV-1 mutant clones (1 triple and 1 sextuple) compared to the wildtype strain. Cross Resistance: Integrase Inhibitor-Resistant HIV-1 Strains: Sixty integrase inhibitor-resistant mutant HIV-1 viruses (28 wi ...
... against 2 non-nucleoside (NN)-RTI-resistant, 3 nucleoside (N)-RTI-resistant, and 2 PIresistant HIV-1 mutant clones (1 triple and 1 sextuple) compared to the wildtype strain. Cross Resistance: Integrase Inhibitor-Resistant HIV-1 Strains: Sixty integrase inhibitor-resistant mutant HIV-1 viruses (28 wi ...
Definition of artemisinin resistance
... Which implications does the identification of the K13 mutation have on the response to artemisinin resistance? There is ‘spreading and popping’. The “firewall approach” remains necessary for tier 1 and 2 areas but additional measures are necessary, which includes an effort for elimination of P. falc ...
... Which implications does the identification of the K13 mutation have on the response to artemisinin resistance? There is ‘spreading and popping’. The “firewall approach” remains necessary for tier 1 and 2 areas but additional measures are necessary, which includes an effort for elimination of P. falc ...
Efficacy of Antiviral Drugs against Feline Immunodeficiency Virus
... require intracellular activation for inhibition of the enzyme [8,42]. NNRTIs are a group of structurally diverse compounds that all bind a single site of the RT [55]. The interaction with the allosteric site which is located in close proximity to the catalytic site, leads to a number of conformation ...
... require intracellular activation for inhibition of the enzyme [8,42]. NNRTIs are a group of structurally diverse compounds that all bind a single site of the RT [55]. The interaction with the allosteric site which is located in close proximity to the catalytic site, leads to a number of conformation ...
Simultaneous Separation of Different Types of Amphetamine and
... final product may contain unreacted starting materials as well as unwanted side reaction products, which are commonly generated during synthesis. Low yield reactions will contain low levels of the drug substance under investigation and may also contain high concentration(s) of by products and/or star ...
... final product may contain unreacted starting materials as well as unwanted side reaction products, which are commonly generated during synthesis. Low yield reactions will contain low levels of the drug substance under investigation and may also contain high concentration(s) of by products and/or star ...
Pharmacy_Lecture_08_..
... Structure-Based Design of Potent Non-Peptide MDM2 inhibitors Structure-Based Design: The p53-MDM2 interaction is primarily mediated by three hydrophobic residues of p53 and a small but deep hydrophobic cleft in MDM2. This cleft is ideal for the design of agents that block the p53MDM2 interaction. Tr ...
... Structure-Based Design of Potent Non-Peptide MDM2 inhibitors Structure-Based Design: The p53-MDM2 interaction is primarily mediated by three hydrophobic residues of p53 and a small but deep hydrophobic cleft in MDM2. This cleft is ideal for the design of agents that block the p53MDM2 interaction. Tr ...
Pharmacometrics and Biostatistics Interactions at the FDA
... • TKV, measured at baseline, is qualified as a prognostic enrichment biomarker – select patients with ADPKD at high risk for a progressive decline in renal function (defined as a confirmed 30% decline in the patient’s eGFR) for inclusion in interventional clinical trials. ...
... • TKV, measured at baseline, is qualified as a prognostic enrichment biomarker – select patients with ADPKD at high risk for a progressive decline in renal function (defined as a confirmed 30% decline in the patient’s eGFR) for inclusion in interventional clinical trials. ...
Eleventh Specialty Pharma Newsletter (December 2009)
... FDA Approves Pomalyst for Advanced Multiple Myeloma. The U.S. Food and Drug Administration today approved Pomalyst (pomalidomide) to treat patients with multiple myeloma whose disease progressed after being treated with other cancer drugs. ...
... FDA Approves Pomalyst for Advanced Multiple Myeloma. The U.S. Food and Drug Administration today approved Pomalyst (pomalidomide) to treat patients with multiple myeloma whose disease progressed after being treated with other cancer drugs. ...
Resistance is futile: the bacteriocin model for addressing the
... of bacterial defence in Nature [14,15]. They are highly specific in their killing action, often active only against close relatives of the producing strains [15]. An ancient family of proteins, routinely employed by microbes to displace competitors and invade novel environments, they remain a viable ...
... of bacterial defence in Nature [14,15]. They are highly specific in their killing action, often active only against close relatives of the producing strains [15]. An ancient family of proteins, routinely employed by microbes to displace competitors and invade novel environments, they remain a viable ...
Structure-based drug design strategies in medicinal
... The combined use of both HTS and SBVS is an important strategy in medicinal chemistry that has allowed the identification of inhibitors of the protein tyrosine phosphatase 1B (PTP1B) (Fig. 3), which plays an important role in metabolism and has been identified as a target for obesity and type II dia ...
... The combined use of both HTS and SBVS is an important strategy in medicinal chemistry that has allowed the identification of inhibitors of the protein tyrosine phosphatase 1B (PTP1B) (Fig. 3), which plays an important role in metabolism and has been identified as a target for obesity and type II dia ...
Nonbeta-lactams_E
... to aminoglycosides. It lacks amino sugars and glycosidic bonds. Spectinomycin is active against many Gram-positive and Gram-negative organisms, but it is used as an alternative treatment for drug-resistant gonorrhea or gonorrhea in penicillin-allergic patients. Strains of gonococci may be resistant ...
... to aminoglycosides. It lacks amino sugars and glycosidic bonds. Spectinomycin is active against many Gram-positive and Gram-negative organisms, but it is used as an alternative treatment for drug-resistant gonorrhea or gonorrhea in penicillin-allergic patients. Strains of gonococci may be resistant ...
Academic paper: A Diarylquinoline Drug Active on the ATP
... proton pump of adenosine triphosphate (ATP) synthase. After AIDS, tuberculosis (TB) is the leading cause of infectious disease mortality in the world, with 2 million to 3 million deaths per year (1). The TB and HIV epidemics fuel one another in coinfected people, and at least 11 million adults are i ...
... proton pump of adenosine triphosphate (ATP) synthase. After AIDS, tuberculosis (TB) is the leading cause of infectious disease mortality in the world, with 2 million to 3 million deaths per year (1). The TB and HIV epidemics fuel one another in coinfected people, and at least 11 million adults are i ...
HIV / AIDS
... Current research and development for HIV is focused on adjunctive therapy, which when combined with existing HAART (Highly Active Anti-Retroviral Therapy) regimens reduce side effects, enhance the efficacy of existing treatments and delay the progression of the HIV virus. The majority of these thera ...
... Current research and development for HIV is focused on adjunctive therapy, which when combined with existing HAART (Highly Active Anti-Retroviral Therapy) regimens reduce side effects, enhance the efficacy of existing treatments and delay the progression of the HIV virus. The majority of these thera ...
Department of Pharmacology
... transport. Loop diuretics; thiazides and thiazide-like drugs; carbonic anhydrase inhibitors; osmotic diuretics; K+-sparing agents. Pharmacokinetics, pharmacodynamics, clinical indications, adverse effects. Antidiuretic hormone antagonists. Case study Introduction: definition of arterial hypertension ...
... transport. Loop diuretics; thiazides and thiazide-like drugs; carbonic anhydrase inhibitors; osmotic diuretics; K+-sparing agents. Pharmacokinetics, pharmacodynamics, clinical indications, adverse effects. Antidiuretic hormone antagonists. Case study Introduction: definition of arterial hypertension ...
NEW_DRUG_APPLICATION
... If the FDA gives the green light, the "investigative" drug will then enter three phases of clinical trials: PHASE 1: uses 20-80 healthy volunteers to establish a drug's safety and profile. (about 1 year) PHASE 2: employs 100-300 patient volunteers to assess the drug's effectiveness. (about 2 yea ...
... If the FDA gives the green light, the "investigative" drug will then enter three phases of clinical trials: PHASE 1: uses 20-80 healthy volunteers to establish a drug's safety and profile. (about 1 year) PHASE 2: employs 100-300 patient volunteers to assess the drug's effectiveness. (about 2 yea ...
Predicting drug pharmacokinetics in humans from in vitro
... dependent clearance of several markers determined by MS was as predicted from the literature. There was a good correlation between the sum of individual CYP Clint and HLM Clint (r# l 0.8, P 0.001) for the substrates, indicating that recombinant CYPs may be used to predict HLM Clint data (Figure 2). ...
... dependent clearance of several markers determined by MS was as predicted from the literature. There was a good correlation between the sum of individual CYP Clint and HLM Clint (r# l 0.8, P 0.001) for the substrates, indicating that recombinant CYPs may be used to predict HLM Clint data (Figure 2). ...
汤慧芳_抗阿米巴_滴虫
... (1)The t½(12~24h) is longer than metronidazole(t½ 8h), (2) After once oral adminis-tration, its effective blood concentration keep 72h, (3) its toxicity is less than metronidazole. ...
... (1)The t½(12~24h) is longer than metronidazole(t½ 8h), (2) After once oral adminis-tration, its effective blood concentration keep 72h, (3) its toxicity is less than metronidazole. ...
ISOA/ARF Drug Development Tutorial
... This tutorial is an introduction aimed at academics and other researchers who are new to the field of drug discovery. We outline here the fundamental concepts and processes of drug discovery. Our goal is to guide researchers toward the steps necessary to translate benchside findings into bedside app ...
... This tutorial is an introduction aimed at academics and other researchers who are new to the field of drug discovery. We outline here the fundamental concepts and processes of drug discovery. Our goal is to guide researchers toward the steps necessary to translate benchside findings into bedside app ...
Identification of novel natural compound inhibitors for human
... Homology modeling of the structure of C5aR A comparative modeling approach was implemented for modeling of C5aR protein of the GPCR family. The 350 amino acid long protein sequence of C5aR (Accession no: P21730) was retrieved from UniProt database in FASTA format. PDB structures sharing a high degre ...
... Homology modeling of the structure of C5aR A comparative modeling approach was implemented for modeling of C5aR protein of the GPCR family. The 350 amino acid long protein sequence of C5aR (Accession no: P21730) was retrieved from UniProt database in FASTA format. PDB structures sharing a high degre ...
GABAMINERGIC NEUROTRANSMISSION: INTRODUCTION
... cofactor. This mechanism is very similar to that described for carbidopa and LAAAD (see Dopamine Biosynthesis Chapter). ...
... cofactor. This mechanism is very similar to that described for carbidopa and LAAAD (see Dopamine Biosynthesis Chapter). ...
FY M.Pharm Medicinal Chemistry
... B. De Novo and fragment based ligand design • Classes of De Novo ligand design – active site analysis methods, whole-molecule methods, connection methods and random connection and disconnection methods. • Fragment based drug design e.g. from literature and programs available to be discussed. C. Phar ...
... B. De Novo and fragment based ligand design • Classes of De Novo ligand design – active site analysis methods, whole-molecule methods, connection methods and random connection and disconnection methods. • Fragment based drug design e.g. from literature and programs available to be discussed. C. Phar ...
The Influence of Conformational Isomerism on Drug
... have an increased duration of action over the parent compound in addition to the above stated advantages. Even though this is an idealized case, it is not that far-fetched. Small, conformationally flexible neurotransmitters such as acetylcholine, norepinephrine and histamine are known to bind in dif ...
... have an increased duration of action over the parent compound in addition to the above stated advantages. Even though this is an idealized case, it is not that far-fetched. Small, conformationally flexible neurotransmitters such as acetylcholine, norepinephrine and histamine are known to bind in dif ...
the chembiobank and eu-openscreen initiatives in chemical
... have boosted an urgent need for new antibacterial agents with novel modes of action.1 In this sense, FtsZ (Figure 1) “a widely conserved tubulin-like GTPase” has recently been proposed as an attractive target for antibacterial drug discovery due to its essential role in bacterial cell division.2 Rec ...
... have boosted an urgent need for new antibacterial agents with novel modes of action.1 In this sense, FtsZ (Figure 1) “a widely conserved tubulin-like GTPase” has recently been proposed as an attractive target for antibacterial drug discovery due to its essential role in bacterial cell division.2 Rec ...
Discovery and development of non-nucleoside reverse-transcriptase inhibitors
![](https://en.wikipedia.org/wiki/Special:FilePath/RTenzyme-hand.jpg?width=300)
Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV). NNRTIs inhibit reverse transcriptase (RT), an enzyme that controls the replication of the genetic material of HIV. RT is one of the most popular targets in the field of antiretroviral drug development.Discovery and development of NNRTIs began in the late 1980s and in the end of 2009 four NNRTI had been approved by regulatory authorities and several others were undergoing clinical development. Drug resistance develops quickly if NNRTIs are administered as monotherapy and therefore NNRTIs are always given as part of combination therapy, the highly active antiretroviral therapy (HAART).