Products

TGHW01AP
Therapeutic Area(s): Parkinson’s disease and Erectile Dysfunction
Phase of Development: IND in preparation

Development Status:
IND in preparation

Product Description
FKP has a goal to develop an Apomorphine pro drug with prolonged therapeutic anti-Parkinson effects suitable for delivery orally (once a day), transdermally (once a week) and as an implant (once every six months). Also the drug should produce near complete relief of Parkinson symptoms without dyskinesias. To this end, FKP has the patent rights to a large series of apomorphine monoesters and mixed esters.

The lead compound, TGHW01AP, is an orally active postsynaptic D1 and D2 agonist. The drug has a similar action to apomorphine without the toxicity and short duration of activity of apomorphine.

In freely moving rats with an indwelling interstitial cannula, TGHW01AP, given orally in enteric coated capsules showed obvious behavioral signs of dopamine stimulation for at least 10 hours. Dopamine and DOPAC measured by HPLC from the cannula showed significant decreases indicating dopamine receptor agonism.

Three studies have been conducted on MPTP lesioned levodopa treated marmoset’s at Dr. Tom Chase’s lab at the NIH. TGHW01AP given orally in an enteric coated capsule produced optimal antiparkison activity for 33 hours. Multiple dosing for 7 days produced excellent results with a 28 hour “on” after the last dose. A pharmacokenitic study in these animals demonstrated blood levels out to 36 hours.

These results indicate that this is an important compound which needs to be moved along quickly. The manufacturing, pharmacology and toxicology are ready for IND preparation.

Clinical Trials
Protocols in development.

Partners
Developmental and marketing partnerships are available.