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Product Portfolio: Intravenous Anesthetics

Home / Available Projects / Product Portfolio: Intravenous Anesthetics

  • Overview
  • Propofol Prodrug
  • Etomidate Derivative
  • Midazolam Derivative
  • Data
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-39611, EL-052, and EL-001). These anesthetics show better pharmacokinetics, significantly lower drug toxicity levels, and other advantages compared to current market leaders.

Pipeline LK-39611: water-soluble prodrug of propofol
EL-052: etomidate derivative
EL-001: midazolam derivative
Drug Modality Small molecule
Indication Anesthesia
Status Preclinical
Patent Granted

Licensing Opportunities

All three intravenous anesthetics programs (LK-39611, EL-052, and EL-001) are currently open for out-licensing opportunities worldwide.

Drug Name LK-39611
Description

LK-39611 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-39611 shows significantly better pharmacokinetics and no formaldehyde release in vivo.

LK-39611 has a high therapeutic index, thus it is a safe anesthetic product with huge market potential.

Target The transient receptor potential cation channel subfamily V member 1 (TRPV1)
Drug Modality Small molecule
Indication Anesthesia
Formulation Freeze-dried powder injection/TBD
Product Category Modified new drug
Mechanism of Action TRPV1 agonists
Status Preclinical
Patent Have been granted in China
Drug Name EL-052
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-052 not only avoids that, but also retains all the advantages of etomidate, thus ensuring safe anesthesia.

Target GABA(A) receptor
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 Preclinical
Patent Have been granted in the US, Europe and China; international patents under PCT are pending
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 GABA(A) receptor
Drug Modality Small molecule
Indication Anesthesia
Formulation Freeze-dried powder injection/TBD
Product Category Innovative drug
Mechanism of Action GABA(A) BZ site receptor agonist
Status Preclinical
Patent Have been granted in the US, Europe and China; international patents under PCT are pending

Effects of EL-052 and Etomidate on Corticosteroid Secretion Inhibition in Canine Model

ACTH (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.


Bispectral Index Score Monitoring of EL-001 and Remimazolam in Rat Model

The 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.

Diane Hong Business Development Manager
1-516-927-7606
info@protheragen.com

Protheragen’s business is growing rapidly after founded in Ronkonkoma, New York in 2009. More offices have been established at different locations across China and the US ever since.

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Email: info@protheragen.com