| Description |
Propofol, midazolam, and etomidate are the most common intravenous anesthetics used in clinical applications today. Unfortunately, the drug formulations that are available on the market still show many disadvantages. Improved prodrugs and derivatives of the most common intravenous anesthetics were developed (LK-396, EL-0052, and EL-001) by the company we have collaborated with, which is engaged in the development of modified new drugs and innovative drug candidates. These anesthetics show better pharmacokinetics, significantly lower drug toxicity levels, and other advantages compared to current market leaders. |
| Pipeline |
LK-396: water-soluble prodrug of propofol EL-0052: etomidate derivative EL-001: midazolam derivative |
| Drug Modality | Small molecule |
| Indication | Anesthesia |
| Status | Preclinical/Phase II (NMPA) |
| Patent | Granted |
All three intravenous anesthetics programs (LK-396, EL-0052, and EL-001) are currently open for out-licensing opportunities worldwide.
| Drug Name | LK-396 |
| Description |
LK-396 overcomes the problem of poor water solubility of propofol, thus avoiding the stimulation at drug’s injection site, caused by the release of propofol from fat emulsion. Compared with another prodrug – propofol phosphate, LK-396 shows significantly better pharmacokinetics and no formaldehyde release in vivo. LK-396 has a high therapeutic index, thus it is a safe anesthetic product with huge market potential. |
| Target | GABAA |
| Drug Modality | Small molecule |
| Indication | Anesthesia |
| Formulation | Freeze-dried powder injection/TBD |
| Product Category | Modified new drug |
| Mechanism of Action | Activation of the GABAA receptor complex |
| Status | Preclinical |
| Patent | Patents have been granted in the US and Europe. |
| Drug Name | EL-0052 |
| Description |
Etomidate is a suitable anesthetic for the elderly and critically ill patients, showing no or little effects on circulation and respiratory system. However, prolonged use of etomidate results corticosteroid synthesis inhibition, significantly increasing surgical mortality. EL-0052 not only avoids that, but also retains all the advantages of etomidate, thus ensuring safe anesthesia. |
| Target | GABAA |
| Drug Modality | Small molecule |
| Indication | Anesthesia |
| Formulation | Intravenous emulsions |
| Product Category | Innovative drug |
| Mechanism of Action | Positive modulation of GABA-mediated activity and direct activation of GABAA receptors |
| Status | Phase II (NMPA) |
| Patent | Patents have been granted in the US, Europe, and Japan. |
| Drug Name | EL-001 |
| Description |
A common midazolam derivative, remimazolam, usually can be toxic by producing genotoxic impurities while in storage, and by producing formaldehyde in patient’s body. EL-001, an ethyl ester hydrochloride derivative of midazolam, does not show any similar toxicities. Animal studies have shown that EL-001 is more effective and has quicker onset of action. In addition, its duration of action and recovery time after withdrawal are both shorter than remimazolam, thus making EL-001 easier to control, and a much better option for the patients in general. |
| Target | GABAA |
| Drug Modality | Small molecule |
| Indication | Anesthesia |
| Formulation | Freeze-dried powder injection/TBD |
| Product Category | Innovative drug |
| Mechanism of Action | GABAA BZ site receptor agonist |
| Status | Preclinical |
| Patent | Patents have been granted in the US and Europe, and international patents under PCT are pending. |
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Effects of EL-0052 and Etomidate on Corticosteroid Secretion Inhibition in Canine ModelACTH (1-24) was administered to stimulate corticosterone secretion in canine model. Corticosterone concentration in serum was then determined. Results showed that corticosterone concentration did not change in the etomidate group, both before and after the administration of ACTH (1-24). However, in the EL-0052 group corticosterone concentration increased significantly after ACTH (1-24) administration, and was higher compared to the etomidate group. |
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Bispectral Index Score Monitoring of EL-001 and Remimazolam in Rat ModelThe bispectral index score (BIS) has been used as an indicator of a sedative state and is related to anesthetic agents and noxious stimulus. BIS was measured after the administration of EL-001 or remimazolam. After bolus infusion, BIS decreased faster in rats administered with EL-001 than with remimazolam. Also, recovery of consciousness was significantly quicker in EL-001-treated rats. |
Protheragen's business is growing rapidly after founded in New York. Our business has evolved from the initial intermediary service to encompass segments in equity investment and program incubation.
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