What is the significance of P-glycoprotein in pharmacokinetics?

The general function of P-glycoprotein is now known to protect the body from harmful substances by: Removing drugs absorbed in the intestines back into the gut lumen. Maintaining the integrity of the blood brain barrier. Removing drugs from the kidneys and liver into the urine and bile respectively.

Is P-glycoprotein the same as MDR1?

MDR1, more commonly referred to as P-gp or P-glycoprotein, is an efflux transporter that serves two major drug transport functions. Firstly, it restricts the distribution of its substrates into organs such as the brain, testes, placenta, and the GIT.

What is the role of P-glycoprotein in multi drug resistant cancers?

P-glycoprotein (P-gp) is a key player in the multidrug-resistant phenotype in cancer. The protein confers resistance by mediating the ATP-dependent efflux of an astonishing array of anticancer drugs.

What anticancer drugs would be affected by P-glycoprotein?

A plethora of anticancer drugs that are central to many chemotherapeutic regimes are susceptible to P-gp-mediated efflux (Figure 1), such as the microtubule-targeting vinca alkaloids (e.g. vinblastine and vincristine) and taxanes (paclitaxel and docetaxel), the DNA-chelating anthracyclines (doxorubicin and daunorubicin …

What does P-glycoprotein do?

P-glycoprotein, the most extensively studied ATP-binding cassette (ABC) transporter, functions as a biological barrier by extruding toxins and xenobiotics out of cells. In vitro and in vivo studies have demonstrated that P-glycoprotein plays a significant role in drug absorption and disposition.

Does azithromycin inhibit P-glycoprotein?

The FDA approved macrolide antibiotics (erythromycin, azithromycin, and clarithromycin) were all reported as p-gp inhibitors. This has been supported by many studies in the literature (64–66).

What anticancer drugs are affected by P-glycoprotein?

Is digoxin a P-gp inhibitor?

Conclusions—Quinidine and digoxin are both substrates for P-glycoprotein, and quinidine is a potent inhibitor of digoxin transport in vitro.

What is P glycoproteins role in multi drug resistant cancers?

What is P-glycoprotein role in multi drug resistant cancers?

How do the P-gp inhibitors work?

In general, P-gp can be inhibited by three mechanisms: (i) blocking drug binding site either competitively, non-competitively (Fig. 2) or allosterically; (ii) interfering with ATP hydrolysis; and (iii) altering integrity of cell membrane lipids.

Is azithromycin a P-gp inhibitor?

The FDA approved macrolide antibiotics (erythromycin, azithromycin, and clarithromycin) were all reported as p-gp inhibitors.