Table 3.
Technologies for oral delivery of proteins under clinical development by companies.
| Company | Product name | Technology | Formulation | Development phase | Product | References |
|---|---|---|---|---|---|---|
| Apollo Life Science | Oraldel™ | Nanoparticles | Tablet | Clinical phase I b | Insulin, TNF-blocker | http://apollolifesciences.com |
| Emisphere | Eligen | Penetration enhancers-Salcaprozate sodium | Tablet | Phase II | Calcitonin, insulin, PTH, heparin, calcitonin, enzymes (lipases, esterases, proteases) | http://emisphere.com |
| Nobex/Biocon | HIM2 | Pegylation + PE | Liquid | Abandoned | Insulin, enkephalin, calcitonin, PTH | Wajberg et al., 2004 |
| Oramed | ORMD-0801 ORMD-0901 |
Salts of EDTA (enteric coated + PE) | Capsule | Phase I | Insulin/Exenatide | Kidron et al., 2004 |
| Diasome pharmaceuticals | Hepatic-directed vesicles-insulin (HDV-1) | Liposomal insulin | Tablet | Phase II/III | Insulin | Schwartz et al., 2008 |
| Diabetology | Capsulin | PE | Capsule | Phase II | Insulin | Whitelaw et al., 2005 |
| Coremed | Intesulin | Nanoparticle encapsulation | Capsule | Preclinical | Insulin | Carino et al., 2000 |
| Merrion pharma (Ireland) with Novo-Nordisk (Denmark) | Vetsulin | PE (sodium caprate {C10}) | Matrix tablet | Phase I | Insulin and GLP-1 analogues | Walsh et al., 2011 |
| Chiasma (Israel) | Octreolin | PE (sodium caprylate{C8}) | Suspension | Phase I (phase I completed, phase III enrolling | Octreotide | http://chiasmapharma.com |
| Unigene/Tarsa (USA) | PeptelligenceTM | PE (Citric acid + acyl carnitine) | pH-dependent coated dosage form | 2011, Phase III completed | Salmon calcitonin | http://tarsatherapeutics.com |
| Altus | CLEC® | Protein crystallization | Tablet | Trial and error approach | Calcitonin and other polypeptides | Margolin (1996) |
| Generex | Oral–Lyn ™ | PE | Spray devices and aerosol particles | Phase IV | Insulin, Macrotonin | http://www.generex.com |
| Endorex | Orasome TM | Polymerized liposome | – | Phase II | Insulin, growth hormones, vaccines | Okada et al., 1998 |
| Provalis PLC | MacrulinTM | Lipid based microemulsion | Emulsion | Phase II | Insulin, Salmon calcitonin | Cilek et al., 2006 |
| Eli–lily | AI-401 | Enzyme inhibitor | Oral formulation | Phase II | Insulin | http://autoimmuneinc.com |
Abbreviations: EDTA, Ethylene diaminetetraacetic acid; PE, Penetration enhancers; PTH, Parathyroid hormone; TNF, Tumor necrosis factor.