Target intelligence / Profile preview

Organic anion transporting polypeptide 2B1, Organic anion transporting polypeptide 1B1, Organic anion transporting polypeptide 1B3 (OATP2B1 (for Solute carrier organic anion transporter family member 2B1), OATP1B1 (for Solute carrier organic anion transporter family member 1B1), OATP1B3 (for Solute carrier organic anion transporter family member 1B3))

Target
OATP2B1 (for Solute carrier organic anion transporter family member 2B1), OATP1B1 (for Solute carrier organic anion transporter family member 1B1), OATP1B3 (for Solute carrier organic anion transporter family member 1B3)
Molecular classification
Transporter, Solute carrier family, Organic anion transporter
01

Overview

Organic anion transporting polypeptide 2B1 (OATP2B1, encoded by SLCO2B1), OATP1B1 (SLCO1B1), and OATP1B3 (SLCO1B3) are members of the solute carrier (SLC) superfamily of membrane transporters that facilitate the uptake of a wide range of endogenous and exogenous organic anions, including drugs, toxins, bile acids, and hormones, across the plasma membrane[1][2][3][4][5]. OATP2B1 is widely expressed, including in the intestine, liver, placenta, and various endothelial tissues, and plays a key role in drug absorption, disposition, and hormone regulation[1][3]. OATP1B1 and OATP1B3 are primarily liver-specific, located on the basolateral (sinusoidal) membrane of hepatocytes, serving as gatekeepers for hepatic drug uptake and subsequent metabolism or excretion[4][6][7]. These transporters exhibit broad substrate overlap but can differ in specificity and tissue distribution. They are clinically important due to their involvement in drug–drug interactions, genetic polymorphism-related variability in drug response, and as determinants of drug-induced toxicities, particularly with statins and chemotherapeutics[1][2][3][7]. Each transporter (OATP2B1, OATP1B1, OATP1B3) should be recorded as an individual target for structured databases. "OATP2B1/1B1/1B3 transporters" is an aggregate term and should not be used as a canonical entry.

Other names
OATP-BOATPBSLC21A9SLCO2B1SLC21A6SLCO1B1SLC21A8SLCO1B3
02

Mechanism of action

Substrate uptake via Na⁺-independent, facilitated diffusion Drug–drug interaction (inhibition or competition can alter drug absorption and clearance)

03

Biological functions

Uptake and transport of organic anion drugs and endogenous compounds (e.g., steroid and thyroid hormone conjugates, bile acids, various statins, anticancer drugs, antibiotics)Regulation of drug absorption and dispositionModulation of steroid hormone and bile acid homeostasis
04

Disease associations

Cancer (modification of drug uptake and resistance)Liver diseases (drug-induced liver injury due to altered transporter function)Other drug-induced toxicities (by influencing pharmacokinetics of substrates)
05

Safety considerations

Drug–drug interactions, especially statin-induced myopathy/rhabdomyolysis when co-administered with OATP inhibitorsGenetic polymorphisms reducing transporter function, affecting drug clearance and toxicity riskOrgan-specific toxicities due to altered disposition of drugs and metabolites
06

Interacting drugs

Statins (atorvastatin, pravastatin, rosuvastatin, simvastatin)

5 more in the full profile.

07

Biomarkers

OATP1B1 and OATP1B3 genotype and protein expression are biomarkers for altered statin and methotrexate pharmacokinetics and toxicity riskEndogenous substrate plasma levels (e.g., estrone sulfate, coproporphyrin I/III for OATP activity)

Beyond the preview

Go deeper on Organic anion transporting polypeptide 2B1, Organic anion transporting polypeptide 1B1, Organic anion transporting polypeptide 1B3 (OATP2B1 (for Solute carrier organic anion transporter family member 2B1), OATP1B1 (for Solute carrier organic anion transporter family member 1B1), OATP1B3 (for Solute carrier organic anion transporter family member 1B3)).

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on Organic anion transporting polypeptide 2B1, Organic anion transporting polypeptide 1B1, Organic anion transporting polypeptide 1B3 (OATP2B1 (for Solute carrier organic anion transporter family member 2B1), OATP1B1 (for Solute carrier organic anion transporter family member 1B1), OATP1B3 (for Solute carrier organic anion transporter family member 1B3)).

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call