PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
lopinavir

2D structure

Overview

Generic Names: ABT-378; LPV
Trade Names: Aluviran; Koletra
Brand Mixtures: Kaletra (Lopinavir + Ritonavir)
PharmGKB Accession Id: PA450264

Description

Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. It is marketed by Abbott as Kaletra, a co-formulation with a sub-therapeutic dose of ritonavir, as a component of combination therapy to treat HIV/AIDS. (source: Drug Bank)

Indication

Indicated in combination with other antiretroviral agents for the treatment of HIV-infection. (source: Drug Bank)

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Lopinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. (source: Drug Bank)

Pharmacology

Lopinavir is an antiretroviral of the protease inhibitor class. (source: Drug Bank)

Food Interactions

Avoid St.John's Wort.
Take with food. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. Lopinavir is extensively metabolized by the hepatic cytochrome P450 system, almost exclusively by the CYP3A isozyme. (source: Drug Bank)

Protein Binding

Lopinavir is highly bound to plasma proteins (98-99%). (source: Drug Bank)

Absorption

Administered alone, lopinavir has insufficient bioavailability; however, like several HIV protease inhibitors, its blood levels are greatly increased by low doses of ritonavir, a potent inhibitor of cytochrome P450 3A4. (source: Drug Bank)

Toxicity

Although human experience of acute overdosage with lopinavir is limited, accidental ingestion of the product by a young child could result in significant alcohol-related toxicity and could approach the potential lethal dose of alcohol. (source: Drug Bank)

Isomeric SMILES Code:

Cc1cccc(c1OCC(=O)N[C@@H](Cc2ccccc2)[C@H](C[C@H](Cc3ccccc3)NC(=O)[C@H](C(C)C)N4CCCNC4=O)O)C (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs1045642 at chr7:86976581 in ABCB1
    Risk or phenotype-associated allele: none. Phenotype: Efavirenz and lopinavir plasma levels. Study size: 67. Study population/ethnicity: HIV patients. Significance metric(s): not available from abstract. Type of association: GN; PK.
    Variant Name:
    ABCB1:3435T>C, Ile1145Ile
    Related Drugs:
    efavirenz, lopinavir
    Evidence:
    PMID:14711599
  2. rs8187710 at chr10:101601284 in ABCC2
    Risk or phenotype-associated allele: A. Phenotype: This SNP in ABCC2 was associated with a higher accumulation of lopinavir in peripheral blood mononuclear cells of HIV-treated patients. Study size: 53. Type of association: GN.
    Related Drugs:
    lopinavir
    Related Diseases:
    HIV Infections
    Evidence:
    PMID:19842932
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
  •   
  •   
  •   
  •   
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ABCC2
  •   
  •   
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP3A
  •   
  •   
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  • CO
  • PD
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
  •   
  •   
  • PK
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ORM1
  •   
  •   
  • PK
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ORM2
  •   
  •   
  • PK
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
SLCO1A2
  •   
  •   
  • PK
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Has annotations
SLCO1B1
  •   
  •   
  • PK
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
SLCO1B3
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
UGT1A1
  •   
  •   
  • PK
  •   
  •   
Publications

A list of non-curated publications that mention this drug along with other genes is available.

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
irinotecan
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ritonavir
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
tenofovir
  •   
  • PD
  • PK
  •   
  •   
Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Cushing Syndrome
  • CO
  • PD
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
HIV
  •   
  •   
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
HIV Infections
  • CO
  • PD
  • PK
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Sarcoma, Kaposi
  •   
  •   
  • PK
  •   
  •   
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Genetic Variants in Protease Inhibitor associated Adverse Events

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01601
KEGG Compound ID:
C12871
KEGG Drug ID:
D01425
PubChem Compound ID:
92727
PubChem Substance ID:
10225535

Common Searches

Search PubMed
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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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