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ivaroxaban and due to this the net clinicalbenefitfavored enoxaparin. Since patients in Magellan constituteda heterogeneous group affected by different diseases, a subgroupanalysis is currently ongoing to identify patients whocould be related with a net clinical benefit.Therapy Trials.EINSTEIN-DVT (-)-MK 801 EVALUATION is aphase III clinical trial comparing rivaroxaban, 15 mg POBID for 3 weeks followed by 20 mg every day, versus enoxaparinfollowed by VKA, for 3 to 12 months, in patients with acutesymptomatic DVT. The results showed that rivaroxabanhad noninferior efficacy with respect to the primaryoutcome that was the prevention of symptomatic recurrentDVT. The rate of bleedingwas equivalent amongst both groups.
EINSTEIN PE can be a phase III clinical trial, completedbut not published however, that (-)-MK 801 compares rivaroxaban 15 mg BIDfor 3 weeks followed by 20mg every day to enoxaparin 40 mg SQBID for at least 5 days, in combination with VKAin the treatment of patients with acute symptomatic PE withor with out symptomatic DVT. The main endpoint is thecomposite of recurrent DVT and/or PE occurring during the3-, 6-, and 12-month study treatment periods.EINSTEIN-EXTENSION study can be a phase III clinicaltrial designed to assess the efficacy and safety of rivaroxaban20 mg every day for 6 to 12 months, versus placebo in patientswho had completed 6 to 12 months of anticoagulant treatmentfor their acute episode of VTE. The incidence of VTEwas 1.3% versus 7.1% for rivaroxaban A 205804 and placebo, respectively. The results demonstrated that rivaroxabanwas related to an 82% relative danger reduction inthe recurrence of VTE in this group of patients.
The rateof bleeding for the rivaroxaban group was low and nonstatisticallysignificant.2.2. PARP Apixaban. Apixaban is another oral, potent, reversible,and direct FXa inhibitor that has been tested for VTE treatmentand prophylaxis. It is an extremely selective drug and likerivaroxaban can inhibit totally free FXa also as prothrombinaseactivity. Apixaban features a high oral bioavailability and aftera fast oral absorption in the stomach and little intestine,reaches a Cmax roughly 1–3 hours soon after administration.Its half-life is 8–15 hours and about 87% is bound toplasma proteins. Apixaban features a multimodal mechanismof elimination. The majority of the drug is excreted in thefeces, other portion through CYP3A4-dependent mechanisms in theliver, and one-fourth from the drug is eliminated in the urine.
For this reason apixaban possibly might be safelyused in patients with renal and hepatic insufficiency; butlike rivaroxaban, its concomitant use with potent CYP3A4inhibitors like ketoconazole and ritonavir, ought to be avoided.The PT and aPTT are prolonged by the use A 205804 of apixabanin a concentration-dependent fashion. However; because attherapeutic concentrations the impact of apixaban on the PTand aPTT is minimal, these tests usually are not sensitive sufficient forthe monitoring from the drug. Generally, if ever required, anFXa inhibition assay may be the very best method to monitor the activity ofapixaban.2.2.1. Clinical Trials of Apixaban in VTE. Apixaban is in theprocess of approval in Europe for prophylaxis soon after majororthopedic surgery. The ADVANCE 1, 2, and 3 trials are thestudies presented to assistance this indication.
Other trials toevaluate apixaban for the prevention of VTE in patients hospitalizedor with metastatic cancer are also ongoing.Principal Prevention Trials.ADVANCE-1 can be a phase IIIstudy that compared apixaban 2.5mg PO BID with enoxaparin30mg (-)-MK 801 SQ BID for prevention of VTE soon after TKR. Bothdrugs had been started 12–24 h soon after operation and also the durationof treatment was 10–14 days. The results showed thatapixaban did not meet the prespecified statistical criteria fornon-inferiority, but its use was associatedwith reduce rates of clinically relevant bleeding and it had asimilar adverse-event profile.ADVANCE-2 can be a phase III clinical trial that comparedapixaban 2.5mg PO BIDwithenoxaparin 40 mg dailyfor preventionof VTE soon after TKR.
The results showed that apixabanhad noninferior efficacy with respect to the main outcomethat was a composite of total VTE plus all-cause mortality. Further, apixaban was associatedwith a equivalent danger of bleeding.ADVANCE-3 can be a phase III clinical trial comparingapixaban 2.5mg PO BIDwithenoxaparin 40 mg dailyfor thromboprophylaxisafter A 205804 THR. The main efficacy outcome,a composite of VTE plus all-cause mortality, occurred in1.4% from the patients in the apixaban group and in 3.9%of the patients in the enoxaparin group. The rates of bleeding inboth groups had been equivalent. It was concluded that among patientsundergoing hip replacement, thromboprophylaxiswith apixaban, as compared with enoxaparin, was associatedwith reduce rates of VTE, with out increased bleeding.ADOPT can be a phase III clinical trial, completed but notpublished however, designed to assess the efficacy and safety ofapixaban, 2.5 gmg POBID versus enoxaparin 40 mg SQ dailyfor prophylaxis of VTE in acutely ill healthcare subjects duringand following hospitalization. The main efficacy outcomeis a composit