Esterom

Esterom is an investigational drug that was studied for use as a topical analgesic. Chemically, it is a mixture of compounds derived from the esterification of cocaine in propylene glycol.^[1] While the major component is benzoylecgonine,^[2] the analgesic activity is likely due to hydroxypropyl benzoylecgonine, the only component that penetrates the skin.^[1]^[3] Clinical trials of Esterom failed so show a statistically significant benefit for patients in 2002 and was never approved.^[4]^[5]

References

↑ ^1.0 ^1.1 "Determination of the dermal penetration of esterom components using microdialysis sampling". Pharmaceutical Research 20 (11): 1827–34. November 2003. doi:10.1023/B:PHAM.0000003381.10208.8c. PMID 14661928.
↑ "Cyclodextrin-modified micellar electrokinetic chromatography for the analysis of Esterom, a topical product consisting of hydrolyzed benzoylecgonine in propylene glycol". Electrophoresis 24 (11): 1764–9. June 2003. doi:10.1002/elps.200305374. PMID 12783453.
↑ "Comparative potency for impulse-blockade and for cutaneous analgesia of traditional and novel local anesthetics.". American Society of Anesthesiology Annual Meeting. 2002. http://w.asaabstracts.com/strands/asaabstracts/abstract.htm?year=2002&index=10&absnum=1331. "...hydroxypropylbenzoylecgonine (HPBE) is the only effective analgesic compound in [Esterom]."
↑ "Benzoylecgonine" (in en). https://go.drugbank.com/drugs/DB01515.
↑ Baron, Michael (2002-09-09). "Entropin dives on disappointing drug" (in EN-US). https://www.marketwatch.com/story/entropin-shares-tumble-on-disappointing-drug-trial.

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[McDonald-1] 1.0 ^1.1 "Determination of the dermal penetration of esterom components using microdialysis sampling". Pharmaceutical Research 20 (11): 1827–34. November 2003. doi:10.1023/B:PHAM.0000003381.10208.8c. PMID 14661928.

[2] "Cyclodextrin-modified micellar electrokinetic chromatography for the analysis of Esterom, a topical product consisting of hydrolyzed benzoylecgonine in propylene glycol". Electrophoresis 24 (11): 1764–9. June 2003. doi:10.1002/elps.200305374. PMID 12783453.

[3] "Comparative potency for impulse-blockade and for cutaneous analgesia of traditional and novel local anesthetics.". American Society of Anesthesiology Annual Meeting. 2002. http://w.asaabstracts.com/strands/asaabstracts/abstract.htm?year=2002&index=10&absnum=1331. "...hydroxypropylbenzoylecgonine (HPBE) is the only effective analgesic compound in [Esterom]."

[4] "Benzoylecgonine" (in en). https://go.drugbank.com/drugs/DB01515.

[5] Baron, Michael (2002-09-09). "Entropin dives on disappointing drug" (in EN-US). https://www.marketwatch.com/story/entropin-shares-tumble-on-disappointing-drug-trial.

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