An orally bioavailable nanoformulation of betulinic acid, for melanoma
Melanoma is cancer that impacts 69,000 Americans each year, killing approximately 7,000 of them annually. Melanoma cases have doubled over the last three decades, and with the increased popularity of tanning bed usage (an activity which has been reported to increase melanoma risk by 70%), the number of cases is expected to soar. Melanoma is a deadly disease in dire need of a medical solution.
Betulinic Acid – A Unique Melanoma-Specific Natural Product
Poor Water Solubility Limiting Full Therapeutic Efficacy
Unfortunately, betulinic acid is quite insoluble; this insolubility has hampered its clinical development and commercial use. Betulinic acid, a potential clinical candidate that came through NCI's RAID mechanism, was abandoned because of lack of oral bioavailability. It was meant for chronic dosing and no viable, nontoxic, IV formulation could be developed.
Several water soluble and prodrug derivatives have been made in recent years, with the most famous being Bevirimat, 3-O-(3',3'-dimethylsuccinyl)-betulinic acid (PA-457). Unfortunately, this efficacy has not yet translated in vivo in the clinic. While some of the variability in clinical results has been correlated with patients' genetic makeup, some of the difficulties have been associated with making the active site of betulinic acid orally bioavailable. The active site of the molecule is the carboxylic acid group since this is the only difference between betulinic acid and its precursor betulin, which is totally inactive.
APH-0201 – Improved Betulinic Acid Drug Delivery and Bioavailability
APH-0201 is betulinic acid nanoparticles in biodegradable polymer nanospheres that will allow transport to the stomach and enhance oral bioavailability.
Betulinic acid, a pentacyclic triterpene and its precursor, betulin are components of the bark of the Betula alba (white birch) tree. The tree is fast-growing and abundant in North America and Europe.
Betulinic acid is manufactured form the bark of this tree by Aphios using our supercritical fluid extraction and chromatography CXP enabling technology platform.
APH-0201 drug nanoparticles can be taken as pills, improving the drug's ability to reach the melanoma cancer cells and reducing hospitalization time and costs.
APH-0201 Benefits and Advantages
We are seeking strategic corporate partners to continue the development of APH-0201, an orally bioavailable nanoformulation of betulinic acid, for melanoma.