Home / Therapies / Insulin Therapy Center / The Promising Future of Oral Insulin 

The Promising Future of Oral Insulin 

Oct 6, 2020
Editor: Steve Freed, R.PH., CDE

Author: Chardae Whitner, 2020 PharmD. Candidate, Lake Erie College of Osteopathic Medicine

Have the challenges of creating an effective oral insulin formulation finally been overcome? 

Good news may be in store for diabetes patients who need insulin therapy but may have a phobia of needles. Oramed Pharmaceuticals is currently in the final stage of phase 2b trial evaluating an oral insulin’s efficacy and safety. The data extrapolated from this trial is revealing promising and positive results. The oral formulation of this insulin, currently named ORMD-0801, is in capsule form.    


Oramed Pharmaceuticals is the first pharmaceutical company to attempt oral insulin that has progressed this far in the trial. The difficulty of developing oral insulin arises from degradation and absorbance factors; once ingested, the body breaks it down, but Oramed Pharmaceuticals uses an enteric coating and special protection that keeps the insulin from degrading through the GI tract and intestinal wall.  The oral insulin is designed to pass through the intestinal wall and into the liver, with the assistance of special absorption enhancers; this is where it will begin the process of working. This mechanism is similar to the natural process of insulin in the body. It is the hope that the development of a commercially available oral insulin will transform the management of diabetes in patients with type 1 and type 2 diabetes.    

Thus far, the data gathered from the study comes from a randomized, double-blind, placebo-controlled trial that analyzed 78 adults with poorly controlled type 2 diabetes who were currently taking oral diabetes medications. Participants were randomly assigned into five groups: 8 mg oral insulin once daily, 8 mg oral insulin twice daily, 16 mg oral insulin once daily, 16 mg oral insulin twice daily, and placebo once daily for 12 weeks.  Statistical analysis from two sites was excluded due to evidence of treatment by center interaction and a statistically significant placebo effect (n=13). The reduction in HbA1c at week 12 was the primary efficacy endpoint. Of the participants included in the analysis, 57 completed the study. 

This study showed that the participants taking the oncedaily and twicedaily 8 mg of oral insulin achieved HbA1c reductions from baseline 0.95% (0.81% with placebo adjustment; P = .028) and 0.95% (0.82% with placebo adjustment; P = .029), respectively. Data for those participants who were taking the 8 mg oral insulin once daily and had an HbA1c of at least 9% at baseline revealed that these subjects experienced a 1.26% reduction in HbA1c by week 12. Participants who were taking the 16 mg oral insulin once and twice daily showed no reduction in HbA1c. The safety profile of ORMD-0801 also proved to be excellent, with no reports of serious adverse event, weight gain, and increased hypoglycemic episodes compared to the placebo.   

This oral insulin formulation has a promising future, according to representatives at Oramed Pharmaceuticals. ”The statistically significant efficacy data,” says Joel M. Neutel, MD, Principal Investigator of the Phase 2b trial, “coupled with a clean safety profile characterized by no reported weight gain, no increase in serious drug-related adverse events, and no hypoglycemia, further support its clinical potential. It further validates the clinical potential of oral insulin to have a highly beneficial impact on the treatment of diabetes worldwide.” 

The recent rise of injectable insulin cost has prevented many patients with diabetes from appropriately dosing as prescribed, or, as estimated, at least 25 percent of patients with diabetes not taking their insulin.  Oramed Pharmaceuticals believes the oral insulin pill cost will be significantly lower than the price of insulin injections.  This provides hope to patients who currently are not managing their diabetes through injectable insulin therapy due to cost. 

The use of oral insulin will also provide physicians with the ability to control their patient’s diabetes better, and with the possibility of initiating insulin therapy early on in the treatment regimen.  

With the successful outcome of the Phase 2 trial, Oramed Pharmaceuticals is ready to begin the process of discussing with the FDA their plan for a Phase 3 trial.  Phase 3 trials will also be initiated by partner Hefei Tianhui Incubator of Technologies Company (HTIT).   

Practice Pearls: 

  • The possibility of oral insulin therapy provides hope to poorly managed patients with diabetes due to needle phobia or fatigue. 
  • With the recent findings from the clinical trial, low-dose oral insulin’s safety profile is excellent, making it more desirable for patients and practitioners.  
  • Oramed Pharmaceuticals is confident that the Phase 3 trial will be successful, and oral insulin will be available commercially soon. 


Healio. “Low-Dose Oral Insulin Safe, Effective in Phase 2b Trial.” Healio, 29 Feb. 2020, www.healio.com/endocrinology/diabetes/news/online/{92e298bf-5fab-47e3-9589-29c0aa2f2565}/low-dose-oral-insulin-safe-effective-in-phase-2b-trial. 

Rubinstein, Carrie. Diabetic Patients Get Ready: An Oral Insulin Capsule That May Soon Be On The Market.Forbes, Forbes Magazine, 27 Feb. 2020, www.forbes.com/sites/carrierubinstein/2020/02/27/diabetic-patients-get-ready-an-oral-insulin-capsule-that-may-soon-be-on-the-market/. 


ChardaeWhitner, 2020 PharmD. Candidate, Lake Erie College of Osteopathic Medicine