Pharmacokinetics binding affinity

Genetic engineering advances in improving the selectivity of therapeutic monoclonal antibodies (mAbs) in terms of their improved pharmacokinetics, binding affinities, specificities, toxicides, and increased half-life. 

Antiemetics can be administered either intravenously or orally in this situation, depending on patient characteristics such as ability to take oral medications, dosage form availability, and cost considerations.5,10 The intravenous and oral routes are equally effective. When used at equipotent doses, the 5-HT3 antagonists have similar efficacy in preventing acute CINV, despite pharmacokinetic and receptor binding affinity differences.5,10,36... 

A series of diamine amides based on the phenoxypropyl amine scaffold was reported. Amide 26 displayed an hH3 Ki of 1 nM and was selective versus other histamine receptors [73]. The chirality was removed via cyclic diamines to produce tetrahydroisoquinolines, tetrahydroquinolines, benzazepines and indolines [74]. The benzazepine 27 displayed picomolar hH3 binding affinity. Pharmacokinetic issues were also identified with this diamine series, with i.v. half-lives of 10-12 h in the rat. A strategy to remove the diamine skeleton and prepare new H3... 

A major challenge in VLS is the appropriate treatment of ionization and tau-tomerization statuses in the input data. Currently there are no software that is able to deal the required corrections automatically [47]. Another utmost dispute remains the simultaneous optimization of both binding affinity and pharmacokinetic properties [39, 46, 48]. 

Peptide-based gene delivery, 334 Peptide nucleic acid (PNA), 73,252 Pharmacokinetics, 409 Polyethyleneimine (PEI), 369 Peptides with thiol groups, 348 Persistence of gene expression, 10,463 Physiological Pharmacokinetics, 423 PNA binding affinity, 75 Poly anion interchange, 179 Poly cations, 164 Polymeric gel, 447 Polyamidoamine (PAMAM), 376 Polyaminomethacrylates, 379 Poly(L-lysine), 336, 369 Poly(vinyl pyrrolidone) (PVP), 382 Prophylactic vaccines, 474... 

Ouantitative Structure-Activity Relationship Ouantitative Structure-Biodegradability Relationship Ouantitative Structure-Pharmacokinetic Relationship Ouantitative Structure-Property Relationship Multiple correlation coefficient and its square Relative Binding Affinity... 

Munson and Rodbard. Estimates of binding affinity are then compared with the binding affinity of natural corticotropin, corticotropin analogues, and more importantly with the drug concentrations of the compound to be evaluated reached in the toxicology studies, or similar pharmacokinetic studies (level of exposure). 

---