Novel oral anticoagulants.

Oral anticoagulants have been used widely for the treatment of venous thromboembolism and stroke prevention. The vitamin K antagonists (VKAs), such as warfarin, have been around for the last 65 years and its efficacy as thromboprophylaxis remained largely unchallenged, at least until recently. Nonetheless, the VKAs have significant limitations with marked inter- and intra-individual variability, requiring regular monitoring and have important food and drug interactions. Thus, there is an unmet need, with the quest for alternative oral anticoagulants with stable pharmacokinetics and pharmacodynamics that do not need monitoring. The novel oral anticoagulants are in 2 broad drug classes - the oral direct thrombin inhibitors and oral factor Xa inihibitors. This review article provides an overview of the pharmacology and describes the most recent published data on clinical trials with the new oral anticoagulants, which are in the more advanced stages of clinical development.

Phloroglucinol derivatives from Hypericum japonicum.

The isolation and identification of a new phloroglucinol derivative (2), a diterpenol (4), together with the known compounds flavesone (1) and sarothralen B (3), from the aerial parts of Hypericum japonicum are reported. Their structures were established by extensive spectral analysis and the structure of (3) has also been confirmed by a single crystal X-ray determination.