Ramesh Jayaraman, Founder-Director, DoseQuantics Consulting Pvt Ltd, India rence:Gabrielsson J, Green AR. 2009. Quantitative pharmacology or pharmacokinetic pharmacodynamic integration should be a vital component in integrative pharmacology. J Pharmacol Exp Ther. 331(3):767-74.
Ramesh Jayaraman, Founder-Director, DoseQuantics Consulting Pvt Ltd, India Translation is defined as the process of turning observations in the laboratory, clinic and community into interventions that improve the health of individuals. In the context of drug discovery, the perception of translation can be vastly different based on the knowledge and experience of scientists in different…
Ramesh Jayaraman, Founder-Director, DoseQuantics Consulting Pvt Ltd, India The process of discovering and developing a drug to obtain marketing approval is lengthy (approximately 8-10 years), risky (approximately 10% success rate), and expensive (average of 1 billion US dollars). Two major reasons for drug attrition in clinical development are lack of optimal pharmacokinetics (PK) and lack…
Ramesh Jayaraman, DoseQuantics Consulting Stage of Cancer Types of Cancer Treatment The treatment of cancer is based on the stage of cancer and its location in the body. The treatment can be one type or a sequence of different types based on the complexity of the cancer. If the tumor is small, it is removed…
Ramesh Jayaraman, Founder-Director, DoseQuantics Consulting Pvt Ltd, India The cytochrome P450 (CYP450) family of enzymes is responsible for the metabolic clearance of a majority of small molecule drugs. Some of the major CYP450 enzymes are CYP3A, CYP2D6, CYP1A, CYP2C9, CYP2C19, CYP2B6 and CYP2E1. For many drugs a single CYP450 can be contribute to the metabolic…
Ramesh Jayaraman, DoseQuantics Consulting Pharmacokinetic parameters estimated in blood, serum and plasma are normally used for interpreting efficacy (pharmacodynamics) and safety of a drug and to establish pharmacokinetic/pharmacodynamic (PK/PD) relationships for identifying the optimum dose and regimen. However, ethical and methodological reasons make it difficult to measure drug concentrations in tissues. As blood or serum…
Ramesh Jayaraman, DoseQuantics Consulting The KRAS (Kirsten Rat Sarcoma) gene is a rat oncogene homolog in humans that drives myriad cell functions through a network of signaling pathways. Cell growth-factors, which signal through receptor tyrosine kinases (RTKs), activate guanine nucleotide exchange factors (GEFs) that accelerate intrinsic RAS exchange activity and the formation of RAS-GTP which…
The male genital tract (MGT) is a site for infection (HIV), cancer (testicular) and disorders (erectile dysfunction). Since it is part of the male excretory and reproductive system it is also vulnerable to toxic effects of drugs. The MGT is a physiological pharmacokinetic compartment consisting of anatomical (blood-testes barrier) and physiological barriers (expression of drug…
Amiodarone is an antiarrhythmic drug indicated for treatment and prophylaxis of ventricular fibrillation (VF)* and hemodynamically unstable congestive ventricular tachycardia (VT)* Pharmacology: Amiodarone is a class III antiarrhythmic drug. Mechanism : Inhibition of potassium rectifier currents responsible for repolarizing the heart during phase 3 of cardiac action potential. K+ channel-blocking effect results in increased action…
Ramesh Jayaraman, DoseQuantics Consulting In anti-bacterial drug discovery and development, preclinical animal models of infection have played a pivotal role in evaluating the translational potential of drug candidates. Drug regulatory agencies review pharmacology data from preclinical animal models of infection for understanding the pharmacokinetic/pharmacodynamic (PK/PD) basis for setting efficacious dose and regimens for phase 2…
