Executive Summary Information
|Toxicities||Steatosis, MOA standard for PXR agonists.|
|Comments||PXR is a highly promiscuous nuclear hormone receptor that up-regulates uptake of fatty acids into the liver via the transporter CD36. Rifampicin is, therefore, pro-steatotic in the presence of high circulating fatty acid levels. PXR agonists also induce a wide profile of xenobiotic-metabolizing enzymes. This induction is the source of major drug-drug interactions in the clinic but is important for in vitro studies only to the extent that it may affect compound levels in repeated dose experiments. Care should be taken to avoid exposure to air to minimize the formation of the reactive quinone form of the compound.|
|Feedback Contact||Gold Compound Working Group (GCWG)|
- In Vivo Data
- LIINTOP Data
- PK-ADME Data
- 'Omics and IC50 Data
- Physical Properties
- Recommended Product and Source
FDA and Label Information
The following link will display all of the currently approved FDA drug products on the market. The web page will contain a table listing all current products by their respective Tradenames and primary active ingredients. The list is navigable by simply clicking on the product of interest, which will in turn list all of the NDA's and ANDA's associated with that product. From here users can click on a specific NDA or ANDA and see documents that have been submitted for the product that the FDA has made available via their website. The types of documents include approval history, letters, reviews and labels.
FDA Approved Products
This next url will perform a search in the FDA's system for all labels for products that contain "Rifampin" as an active ingredient.
FDA Label Search
The following resource link will perform a PubMed query for the terms "Rifampin" and "liver toxicity".
The table listed below contains a summarized listing of toxic effect information leveraged from the 6th European Framework Programme project LIINTOP. For a complete listing of the Gold Compound evaluation criteria please see the Gold Compound Evaluation and Comments immediately following the summary table below.
|Summary Hepatotoxic Effects from the LIINTOP FP6 Program|