Drotrecogin alfa
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| AHFS/Drugs.com | Monograph |
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| Routes of administration |
i.v. application only |
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| Pharmacokinetic data | |
| Bioavailability | 100% (i.v. application only) |
| Metabolism | endogenous plasma protease inhibitors |
| Biological half-life | less than 2 hours |
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| Chemical and physical data | |
| Formula | C1786H2779N509O519S29 |
| Molar mass | 55000 g/mol |
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Drotrecogin alfa (activated) (Xigris, marketed by Eli Lilly and Company) is a recombinant form of human activated protein C that has anti-thrombotic, anti-inflammatory, and profibrinolytic properties. Drotrecogin alpha (activated) belongs to the class of serine proteases. Drotrecogin alfa has not been found to improve outcomes in people with severe sepsis. The manufacturer's aggressive strategies in marketing its use in severe sepsis have been criticized. On October 25, 2011, Eli Lilly & Co. withdrew Xigris from the market after a major study showed no efficacy for the treatment of sepsis.
Drotrecogin alfa does not improve mortality in severe sepsis or septic shock but does increase bleeding risks. Therefore, a 2011 Cochrane review recommended that clinicians and policymakers not recommend its use.
The following patients should not receive drotrecogin:
The following patients are at an increased risk for bleeding complications due to drotrecogin-alpha therapy, and a careful risk/benefit assessment should be made prior to initiating therapy.
Eli Lilly has recently issued 3 important additional warnings:
Although patients at high risk of bleeding were excluded from the phase III clinical study (PROWESS), 25% of patients treated with drotrecogin and 18% of those receiving placebo experienced at least one bleeding event (principally ecchymoses or GI bleeding) during the 28-day study period. During treatment serious bleeding events (e.g., intracranial hemorrhage, any life-threatening bleeding event, any bleeding event requiring administration of at least 3 units of packed red blood cells daily for 2 consecutive days) occurred in 2.4% of patients treated with drotrecogin and in 1% of those receiving placebo. No significant differences between geriatric patients and younger patients regarding bleeding events in the drotrecogin group have been found.
No other side-effects have been observed so far.
In the meantime a second study encompassing approximately 2,000 adult patients has been completed and the results showed a comparable side-effect profile.
Drug interactions with drotrecogin have not been systematically studied in patients with severe sepsis. Caution should be exercised when using other drugs that affect hemostasis concomitantly with drotrecogin (e.g. aspirin, warfarin, clopidogrel). However, the use of low dose prophylactic Heparin did not affect safety when given concurrently with drotrecogin.
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