Deferasirox

In a recent patent application, mice treated with a related iron chelator, deferasirox (DFS), showed reduced body weight while on a high fat diet compared to untreated controls. Additionally, DFS was claimed to improve whole body metabolism and energy expenditure as measured by increased 02 consumption and C02 production as well as a reduction in white adipose and visceral fat, despite little difference between food intake in the control and treated animal groups [25]. 

Deravirdine (Rescnptor) [Antiretroviral/NNRTI] Uses HIV Infxn Action Nonnucleoside RT inhibitor Dose 400 mg PO tid Caution [C, ] CDC recommends HIV-infected mothers not to breast-feed (transmission risk) w/ renal/hepatic impair Contra Use w/ drugs dependent on CYP3A for clearance (Table VI-8) Disp Tabs SE Fat redistribution, immune reconstitution synd, HA, fatigue, rash, T transaminases, N/V/D Interactions T Effects W/ fluoxetine T effects OF benzodiazepines, cisapride, clarithromycin, dapsone, ergotamine, indinavir, lovastatin, midazolam, nifedipine, quinidine, ritonavir, simvastatin, terfena-dine, triazolam, warfarin effects W/ antacids, barbiturates, carbamazepine, cimetidine, famotidine, lansoprazole, nizatidine, phenobarbital, phenytoin, ranitidine, rifabutin, rifampin effects OF didanosine EMS Use of benzodiazepines and CCBs should be avoided may cause a widespread rash located on upper body and arms OD May cause an extension of nl SEs symptomatic and supportive Deferasirox (Exjade) [Iron Chelator] Uses Chronic iron overload d/t transfusion in pts >2 y Action Oral iron chelator Dose Initial 20 mg/kg... 

Deferasirox dispersible tablet For chronic iron overload due to blood transfusion... 

The oral iron chelator deferasirox is approved for treatment of iron overload. Deferasirox appears to be as effective as deferoxamine at reducing liver iron concentrations and is much more convenient. However, it is not clear yet whether deferasirox is as effective as deferoxamine at protecting the heart from iron overload. 

Deferasirox Orally administered iron chelator for treatment of hemochromatosis that is not adequately treated by phlebotomy ... 

Deferasirox is a tridentate chelator with a high affinity for iron and low affinity for other metals, eg, zinc and copper. It is orally active and well absorbed. In the circulation, it binds iron, and the complex is excreted in the bile. Deferasirox was recently approved for the oral treatment of iron overload caused by blood transfusions, a problem in the treatment of thalassemia and myelodysplastic syndrome. 

ANTACIDS CONTAINING ALUMINIUM DEFERASIROX 1 levels of deferasirox L absorption Avoid co-administration (manufacturers recommendation)... 

The manufacturers of the oral iron chelator deferasirox note that, although concurrent use with vitamin C has not been formally studied, doses of vitamin C up to 200 mg daily were allowed in clinical studies of deferasirox without adverse consequences. ... 

Exjade (Deferasirox). Novartis Pharmaceuticals UK Ltd. UK Summary of product characteristics, August 2006. 

Deferasirox did not alter the pharmacokinetics of digoxin. Food increases the bioavailability of deferasirox, and it should be taken on an empty stomach. The use of deferasirox with aluminium antacids is not recommended. Rifampicin, phenobarbital and pheny-toin are predicted to increase the metabolism of deferasirox, and, until more is known, concurrent use should be monitored. Based on in vitro data, deferasirox might inhibit the metabolism of CYP2C8 substrates like paclitaxel and repaglinide. Hydroxycar-bamide does not alter deferasirox metabolism. 

Although concurrent use has not been formally studied, the manufacturer recommends that deferasirox is not taken with aluminium-containing antacids. - Deferasirox has a lower affinity for aluminium than for iron, but theoretically aluminium might reduce the efficacy of deferasirox. 

In vitro studies suggested that the only cytochrome P450 isoenzyme that was inhibited by deferasirox at concentrations similar to those that might be achieved clinically was CYP2C8. For this reason, the EMEA have re-... 

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