Improved Oral Delivery

Improved Oral Delivery with Eligen®

Oral Salmon Calcitonin (sCT)

  • Inhaled salmon calcitonin has been used for as treatment for osteoporosis.
  • A combination of sCT and 5-CNAC was investigated in Phase III studies for the treatment of both osteoporosis or osteoarthritis.  Phase II studies has shown positive effects on biomarkers for individuals with either of these diseases.
  • Novartis reported Phase III results on these studies which showed some of the expected effects but did not meet the primary endpoints of all the three trials.  For instance, the osteoporosis trial showed the expected positive effect on bone mineral density, but did not reduce fractures.

Oral GLP-1 and PYY

  • GLP-1 and PYY are peptide hormones that are proposed to be useful for the treatment of obesity
  • The two native peptides were combined with Emsiphere’s SNAC carrier in a series of human clinical trials.
  • The trials showed both could be delivered orally in therapeutic amounts.  These studies also showed that these two agents had a positive effect on the amount of food consumed and that the combination of both peptides had a larger effect than either one alone.

Oral Gallium

  • Gallium compounds are bone-targeting agents that are potent inhibitors of bone breakdown and may be useful for diseases associated with accelerated bone loss.
  • Oral bioavailability of gallium is low.
  • A Phase I clinical trial successfully resulted in significant increase in the oral BA of gallium.

Oral Heparin and Low Molecular Weight Heparin (LMWH)

  • Heparin therapy is commonly used the prevention of blood clot formation following major surgical procedures lasting longer than 30 minutes. LMWH products are indicated for prevention of Deep Venous Thrombosis (DVT) after hip or knee replacement surgery as well as other conditions
  • Eligen Technology has demonstrated therapeutic levels of heparin can be reached has shown comparable efficacy to injected Lovenox.

Oral Human Growth Hormone

  • Human Growth Hormone (hGH) is a protein hormone that stimulates tissue growth and is responsible for linear, skeletal, organ, and cell growth.
  • In a small proof of concept study, 8 GHD patients were given oral rhGH. Novartis investigated pharmacokinetics as well as the pharmacodynamic properties of the orally-delivered rhGH. The study showed that growth hormone peaks were recorded in all patients. An increase in IGF-I was seen in some patients, leading to a statistically significant increase in mean serum IGF-I at day 7  addition,

Oral Parathyroid Hormone

  • PTH-1-34 is an injectable peptide for the treatment of women with postmenopausal osteoporosis.
  • A combination of human PTH-1-34 and the absorption enhancer 5-CNAC using Emisphere’s proprietary Eligen® Technology has been investigated in a Phase I study to assess the bioavailability profile of increasing doses of PTH-1-34 administered orally.
  • Novartis reported results of this study which showed potentially relevant therapeutic exposure and safety profiles similar to those of the currently available injectable dosage form.

Improved Oral Ibandronate

  • Ibandronate is a potent bisphosphonate that has been shown to significantly increase bone mineral density and decrease the risk of osteoporotic fractures in post-menopausal women.
  • Its low and highly variable oral bioavailability results in inconveniences for many patients.
  • Application of Eligen Technology resulted in a rapid, more than six-fold increase in oral bioavailability
  • A lower dose of ibandronate should lead to a decrease in adverse events, along with a shorter time to wait before eating could increase compliance


  • Naproxen is an effective NSAID but is not rapidly absorbed; Tmax is around 90 min.
  • Eligen® Technology produced a faster absorption (about half the normal Tmax).  Thus the onset of action of naproxen is expected to be much quicker as well.