Finally, a novel cyclodextrin derivative in human clinics again!

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Breaking news!
Alveron Pharma announced that it has completed a Phase 1 clinical study for OKL-1111, a new drug for the rapid treatment of Intracranial Haemorrhage (ICH) and other life-threatening bleeds associated with the use of anticoagulants or platelet inhibitors. OKL-1111 was well-tolerated in the trial with healthy human volunteers and showed no more adverse events above those in the placebo groups. Volunteers also received an anticoagulant and a pharmacodynamic effect was observed with OKL-1111 administration. In the prior non-clinical program, the drug reduced bleeding in a clinically relevant intracranial haemorrhage model using high doses of an anticoagulant. Furthermore, a broad-spectrum mode of action was demonstrated against all classes of anticoagulant and one platelet inhibitor to date in a standard haemostasis model.
Congratulations! Way to go!

Alveron Pharma completes successful first-in-human trial of OKL-1111

OKL-1111, A modified cyclodextrin as a potential universal reversal agent for anticoagulants

drug discovery,

The fantastic story of a novel cyclodextrin API.
Antithrombotic therapy is inevitably associated with a risk of bleeding and these bleeding complications can be life-threatening. Recently, specific reversal agents were developed for the direct factor Xa and thrombin inhibitors (DOACs). However, next to the fact that these agents are relatively expensive, the use of selective reversal agents complicates the treatment of bleeding patients in practice. A class of cyclodextrins with procoagulant properties was recently discovered. the lead compound being OKL-1111.
OKL-1111 concentration-dependently reversed the in vitro anticoagulant effects of dabigatran, rivaroxaban, apixaban, and edoxaban in the thrombin generation assay. Also, in the absence of a DOAC, OKL-1111 concentration-dependently accelerated coagulation in this assay but did not initiate coagulation. The reversal effect was also seen for all DOACs in the rat tail cut bleeding model. In addition, when tested with other anticoagulants, OKL-1111 also reversed the anticoagulant effect of the vitamin K antagonist warfarin, the low molecular weight heparin enoxaparin, the pentasaccharide fondaparinux and the platelet inhibitor clopidogrel in vivo. OKL-1111 did not have prothrombotic effects in the Wessler model.

Alveron Pharma – Okklo Life Sciences – Sanquin
Joost Meijers, Kamran Bakhtiari, Alex Zwiers, Stephan Peters

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