Transcrocetin – a naturally occurring oxygenation enhancer.

Crocetin is a natural carotenoid and kosmotropic agent found in saffron and the cape jasmine plant.

TSC has been shown to transiently enhance oxygenation in plasma and interstitium.

OXYGENATION

TSC improves oxygenation in a rat ARDS model

INFLAMMATORY PATHWAYS

Crocetin surpasses NF-kB related inflammatory pathways in an ARDS model

HEMORRHAGIC SHOCK

TSC improves vital signs, organ function, and survival in a hemorrhagic shock rat model

ISCHEMIC STROKE

TSC improves oxygenation of brain tissue and reduces the size of infarct in rat and rabbit models of ischemic stroke

DAMAGE INHIBITION

Crocetin inhibits damage to the endothelium and reduce associated inflammation in HUVEC model

LPS-INDUCED ARDS

Crocetin improves the pulmonary vascular damage in the lungs of mice with LPS-induced ARDS and inhibit the inflammatory signaling pathways

  • Pricing 2 – Insights

    LEAF-4L6715 – Liposomal Formulation of TC Resolves Limitations of Free TC to Effectively Treat Hypoxia

    Proprietary liposomal encapsulation design extends transcrocetin circulation and enables localized controlled release, enhancing living tissue oxygenation to overcome hypoxia.

SMALLEST BLOOD VESSELS

Prolonged circulation and controlled release increases accumulation in the smallest blood vessels (microcirculation within hypoxic tissues)

MICROCIRCULATORY TISSUE

Macrophage-assisted delivery enhances accumulation in remote hypoxic microcirculatory tissue and deep organ microenvironments

INCREASED RETENTION

Further retention of the medicine in the damaged microcirculatory tissue due to enhanced permeability and retention (EPR) effect

LEAF-4L6715

  • Origins

    Free transcrocetin is a diterpenoid and natural carotenoid found in spices such as saffron, a constituent of the crocus flower and cape jasmine. Saffron, as a spice, has been consumed in many cultures for thousands of years.

  • Limitations

    Therapeutic use of free transcrocetins has been limited by their
    poor stability and low solubility which limits the bioavailability of transcrocetin. This is further compounded by a short in vivo half-life which limits the pharmacological effect of oxygenation.

  • Design

    LEAF-4L6715 is a carefully crafted liposomal formulation of transcrocetin achieved by entrapping a less soluble, divalent salt of transcrocetin inside the liposome. This construct facilitates the controlled release of transcrocetin from the liposome into blood circulation.

  • Impact

    By releasing transcrocetin into circulation in a controlled manner, LEAF-4L6715 produces a more sustained oxygenation effect.

Transcrocetin – a naturally occurring oxygenation enhancer

Crocetin is a natural carotenoid and kosmotropic agent found in saffron and the cape jasmine plant. TSC has been shown to transiently enhance oxygenation in plasma and interstitium.

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  • Mwchanism of Action

    Mechanism of Action

    Transcrocetin belongs to the class of molecules known as kosmotropes. The hallmark of kosmotropes is to alter the structure of water molecules in aqueous solutions such as water or blood. This altering creates channels through which smaller molecules such as oxygen and glucose can more easily travel to reach tissues where oxygen is needed.

    • Proprietary nano liposomal encapsulation design extends transcroetin circulation and enables localized controlled release, enhancing living tissue oxygenation to overcome hypoxia
    • Prolonged circulation and controlled release increases accumulation in the smallest blood vessels (microcirculation)
    • Macrophage-assisted delivery enhances accumulation in remote hypoxic microcirculatory tissue and deep organ micro-environment
    • Further retention of the medicine in the damaged microcirculatory tissue due to enhanced permeability and retention (EPR) effect
    • Transcrocetin has been nicknamed “The Moses Molecule” because of its kosmotropic ability to part water

We Are Responding

LEAF-4L6715 is currently being studied in a Phase III registrational study in patients with ARDS in Europe via the Cardiovascular European Research Center (CERC).

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