Abacavir ADME
Sub-pathways within Pathway: Abacavir ADME :
Abacavir ADME:
Abacavir is a nucleoside analogue reverse transcriptase inhibitor with antiretroviral activity, widely used in combination with other drugs to treat HIV-1 infection (Yuen et al. 2008). Its uptake across the plasma membrane is mediated by organic cation transporters SLC22A1, 2, and 3; the transport proteins ABCB1 and ABCG2 mediate its efflux. Abacavir itself is a prodrug. Activation requires phosphorylation by a cytosolic adenosine phosphotransferase and deamination by ADAL deaminase to yield carbovir monophosphate. Cytosolic nucleotide kinases convert carbovir monophosphate to carbovir triphosphate, the active HIV reverse transcriptase inhibitor. Abacavir can be glucuronidated or oxidized to a 5'-carboxylate; these are the major forms in which it is excreted from the body.
Drug ADME:
Pharmacokinetics (PK) is a branch of pharmacology dedicated to determining the chemical fate of substances in living organisms, from administration to elimination from the body. PK can be described as how an organism affects a drug, whereas pharmacodynamics (PD) is the study of how a drug affects the organism. Both PK and PD are described for each drug annotated in the Drug Absorption, Distribution, Metabolism and Excretion (ADME) pathways. For example, although paracetamol ADME (PK) is described in this section, the pharmacological inhibition (PD) of its targets (PTGS1 and PTGS2) is described in the relevant pathway where these enzymes perform their physiological duties. A connection is made between the two pathways to link PK and PD annotations.
The disposition of a pharmaceutical compound within an organism can be described by four main stages; absorption, distribution, metabolism, and excretion, abbreviated to ADME (Pallasch 1988, Ruiz-Garcia et al. 2008, Currie 2018). Sometimes, separate steps can be tacked on to ADME depending on what is being described. For example, where a drug is released from a pharmaceutical formulation, liberation (L) is added to ADME (LADME) or where the toxicity of a compound is described, T is added (ADMET).
ADME of various drugs is annotated in this section.
The disposition of a pharmaceutical compound within an organism can be described by four main stages; absorption, distribution, metabolism, and excretion, abbreviated to ADME (Pallasch 1988, Ruiz-Garcia et al. 2008, Currie 2018). Sometimes, separate steps can be tacked on to ADME depending on what is being described. For example, where a drug is released from a pharmaceutical formulation, liberation (L) is added to ADME (LADME) or where the toxicity of a compound is described, T is added (ADMET).
ADME of various drugs is annotated in this section.