Last update 11 Dec 2024

Propofol

Last update 11 Dec 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

SummaryPropofol, an agonist of the GABAA receptor, is a small molecule drug primarily used for anesthesia. Originating from AstraZeneca, propofol gained approval for use in October 1989. Due to its quick onset and short duration of action, propofol has become a popular sedative-hypnotic agent for both induction and maintenance of anesthesia. In addition to its anesthetic properties, propofol has been found to have antiemetic properties and can be used as an adjunct therapy for postoperative nausea and vomiting. While propofol offers therapeutic benefits, it also has a potential for misuse and abuse due to its ability to induce deep sedation or unconsciousness at high doses. Despite its established uses, the precise mechanism of action of propofol is not yet fully understood, and further research is needed to elucidate its pharmacology.

Drug Type

Small molecule drug

Synonyms

Profofol, Propofol Medium and Long Chain Fat Emulsion, 丙泊酚中/长链脂肪乳

+ [20]

Target

GABAA receptor

Mechanism

GABAA receptor agonists(Gamma-aminobutyric acid A receptor agonists)

Therapeutic Areas

Other Diseases

Active Indication

Anesthesia

Inactive Indication

Sedation

Originator Organization

Fresenius Kabi USA LLC

Active Organization

Xi'an Libang Pharmaceutical Co. Ltd.Fresenius Kabi Deutschland GmbHSandoz AG

+ [1]

Inactive Organization

Shanghai Institute of Pharmaceutical Industry

Beijing Sciecure Pharmaceutical Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

US (02 Oct 1989),

Anesthesia

RegulationEmergency Use Authorization (US)

Structure

Molecular FormulaC12H18O

InChIKeyOLBCVFGFOZPWHH-UHFFFAOYSA-N

CAS Registry2078-54-8

1,945

Clinical Trials associated with Propofol

IRCT20190813044521N1 / SuspendedNot ApplicableIIT

The effect of the Bispectral Index (BIS) during induction of anesthesia on the amount of propofol in patients undergoing various surgical procedures.

Start Date22 Dec 2640

Sponsor / Collaborator-

NCT04291521 / Not yet recruitingNot ApplicableIIT

Prospective Study of Induction Medications Used in the Rapid Sequence Intubation of Trauma Patients and a Comparison of Effects on Outcomes

To compare the outcomes of the use of propofol, etomidate, and ketamine as induction agents for adult trauma patients undergoing intubation within 24 hours of admission. The primary goal is to determine the ideal agent that should be used in this patient population for intubations.

Start Date01 Jan 2026

Sponsor / Collaborator

University of Southern California

[+4]

ChiCTR2400093095 / SuspendedPhase 4IIT

The research of opioid-free anesthesia with magnesium sulfate and propofol in elderly undergoing painless gastroenteroscopy

Start Date01 Dec 2024

Sponsor / Collaborator-

100 Clinical Results associated with Propofol

100 Translational Medicine associated with Propofol

100 Patents (Medical) associated with Propofol

25,142

Literatures (Medical) associated with Propofol

01 Apr 2025·DEN open

Sedative effects of propofol and risk factors for excessive sedation in the endoscopic treatment of biliary and pancreatic diseases

Article

Author: Chatto, Mark ; Yamashige, Daiki ; Hijioka, Susumu ; Hara, Hidenobu ; Hagiwara, Yuya ; Agarie, Daiki ; Fukuda, Soma ; Yagi, Shin ; Saito, Yutaka ; Okamoto, Kouhei ; Okusaka, Takuji ; Nagashio, Yoshikuni ; Takasaki, Tetsuro ; Morizane, Chigusa ; Sone, Miyuki ; Maruki, Yuta

Abstract:

Objectives:

The safety and effectiveness of propofol in more complex endoscopic procedures, such as endoscopic retrograde cholangiopancreatography, remain unknown. Thus, we aimed to evaluate propofol sedation during endoscopic cholangiopancreatography, ultrasound‐guided intervention, and gastroduodenal stenting and examine risk factors for excessive sedation.

Methods:

We retrospectively analyzed data from 870 patients who underwent endoscopic treatment with propofol sedation for biliary and pancreatic disease between October 2020 and September 2021. Sedation included propofol and fentanyl, with continuous monitoring of vital signs and the bispectral index. The assessed risk factors included age, complications, body mass index, treatment duration, and specialty.

Results:

Distal bile duct treatment (n = 367), hilar bile duct treatment (n = 197), post‐small‐intestinal reconstruction treatment (n = 75), endoscopic ultrasound‐guided intervention (n = 140), and gastrointestinal obstruction treatment (n = 91) were performed. The rates of excessive sedation, hypoxemia, and hypotension were 7.8%, 6.0%, and 1.8%, respectively. Post‐small‐intestinal reconstruction treatment had the highest incidence rate of excessive sedation (16%), whereas endoscopic ultrasound‐guided intervention had the lowest incidence rate (4.3%). Multivariate analysis revealed significant associations between excessive sedation and comorbid sleep apnea, obesity, and prolonged procedural time.

Conclusions:

Obesity, sleep apnea syndrome, and prolonged procedure time are risk factors for excessive sedation related to propofol use. Thus, sedation techniques should be tailored for these patients.

01 Apr 2025·DEN open

Propofol sedation safety concerns in pediatric endoscopy: Special considerations in the Japanese medical environment

Article

Author: Murakami, Daisuke ; Yamato, Masayuki

01 Apr 2025·DEN open

Comparison of propofol‐based sedation and midazolam sedation in pediatric bidirectional endoscopy conducted by pediatric gastroenterologists

Article

Author: Kurasawa, Shingo ; Horiuchi, Akira ; Nishimoto, Satomi ; Ukai, Satoshi ; Kudo, Takahiro ; Horiuchi, Ichitaro

Abstract:

Objectives:

The effectiveness and safety of propofol‐based sedation and midazolam sedation in pediatric bidirectional endoscopy were compared.

Methods:

We retrospectively analyzed the cases of pediatric patients (≤15 years old) who had undergone bidirectional endoscopy, esophagogastroduodenoscopy, and colonoscopy by pediatric gastroenterologists. Demographic data, indications, sedatives/dosages, clinical outcomes, endoscopic findings, adverse events, and total patient time requirements (total time in which patients stay in our hospital) were compared in the two sedation groups.

Results:

Ninety‐one children (51 boys, 40 girls, mean age 13 years, range 9–15) treated at our hospital were enrolled. Propofol alone or in combination with midazolam and/or pentazocine was administered to 51 patients (propofol‐based sedation group). Midazolam alone or in combination with pentazocine was administered to the other 40 patients (midazolam sedation group). In the propofol group, the following mean doses were used: propofol, 96 mg (range 40–145 mg); midazolam, 4.9 mg (range 3–5 mg); and pentazocine, 7.5 mg. In the midazolam group, the mean doses of midazolam and pentazocine were 6.2 mg (range 4–10 mg) and 15 mg, respectively. All procedures were successfully completed by pediatric gastroenterologists. The total procedure times and endoscopic findings were similar in the two groups, but the median patient time requirement in the propofol group was significantly shorter versus the midazolam group (7.3 h vs. 8.4 h, p < 0.001). No adverse events occurred in either group.

Conclusions:

Propofol‐based sedation in pediatric bidirectional endoscopy was safely and effectively performed by pediatric gastroenterologists, and its patient time requirement was shorter than that for midazolam sedation.

News (Medical) associated with Propofol

10 Dec 2024

·www.echemi.com

Remarkable Sales Discrepancy of Remimazolam: $40 Million in China, Only $800,000 in the U.S.

In recent years, among the new anesthetic sedation drugs launched on the market, Remazolam has undoubtedly aroused widespread concern in the industry. The drug was designed and synthesized by GlaxoSmithKline (GSK) in 1999, and after several corporate transfers, it was approved for market in China, the United States, Europe and other countries and regions around 2020. However, there are significant differences in the market performance of remazolam across countries. According to 2023 data, the drug's sales in China are about $40 million, while in the United States it is only $800,000, accounting for only 2% of the Chinese market. The reasons for this difference are worth exploring in depth. Remazolam is an ultra-short-acting GABAA receptor agonist whose design is inspired by midazolam and remifentanil, combining the properties of both. It is rapidly metabolized by carboxylesterases in the liver to produce inactive metabolites, resulting in rapid sedation resolution and short sedation recovery time. Remazolam's development history dates back to 1999, when GSK designed and synthesized the drug based on remifentanil's properties and filed a patent application. The patent was then transferred to TheraSci in the United Kingdom. Paion began developing the drug in 2008. Due to the instability of remazolam's free base, Paion developed remazolam benzenesulfonate, while Hengrui Pharmaceuticals adopted remazolam in the form of (toluene sulfonate) salt. At present, these two salt types of remazolam have been listed, of which Remazolam toluene sulfonate is only listed in China, while Remazolam benzenesulfonate is listed in China, Japan, the United States, Europe and other countries, but there are differences in indications. In the Chinese market, RenFCM obtained the Chinese market rights of Remazolam besylate in 2012, and was approved by the State Food and Drug Administration for sedation in colonoscopy in 2020, followed by the induction and maintenance of general anesthesia and the indication of bronchoscopic sedation. In the United States, Remazolam besylate was approved in July 2020 under the trade name Byfavo for a 30-minute sedation procedure marketed by Eagle. Remazolam besylate is approved for induction and maintenance of general anesthesia in Japan and South Korea. It is worth noting that in the first quarter of 2024, Paion was acquired by China's Renfu Pharmaceutical, which means that the global interests of Remazolam besylate have been vested in Renfu Pharmaceutical. Remazolam toluene sulfonate was first approved for sale in China in 2019 for indications including induction and maintenance of general anesthesia and sedation during colonoscopy. The difference in sales in the U.S. and China markets may be related to the different range of indications approved for remazolam in different countries. In the United States, Remazolam is only approved for procedural sedation, while in China, its approved indications include general anesthesia and sedation, and sales are significantly higher than in the United States. In addition, the difference in sales performance between China and the United States may also be related to concerns about remazolam metabolites. Remazolam is metabolized in the body to produce methanol, which may be further oxidized to formaldehyde and formic acid, and formaldehyde is potentially cytotoxic. As a result, the FDA requires remazolam to be administered only within 0.5 hours to avoid the buildup of methanol and its metabolites to dangerous levels. At present, other anesthetic sedatives commonly used in clinical practice, such as propofol, benzodiazepines (represented by midazolam), and α-receptor agonists (represented by dexmetropil), all have their own shortcomings. Although Remazolam still has room for improvement in some aspects, its unique advantages, such as rapid onset, rapid metabolism, rapid sedation recovery, etc., make it a potential application value in the field of anesthesia sedation. With the advancement of medical technology and the in-depth exploration of clinical applications, there may be an improved version of remazolam in the future, bringing new options to the field of anesthesia sedation.

Drug ApprovalAcquisitionPatent ExpirationBiosimilar

14 Nov 2024

·www.accesswire.com

Enalare Therapeutics is Granted a New Patent for ENA-001, Extending Its Exclusivity in the U.S. to 2043

The New Patent Covers ENA-001 Methods of Treating Respiratory Depression Caused by Propofol, a Widely Used, Centrally Acting AnestheticPRINCETON, NJ / ACCESSWIRE / November 14, 2024 / Enalare Therapeutics Inc., a clinical-stage biopharmaceutical company dedicated to developing novel compounds for the treatment of life-threatening critical care conditions and community health emergencies, today announced that the U.S. Patent and Trademark Office (USPTO) has granted U.S. Patent No. 12,138,267 on November 12, 2024, titled, "Methods of Treating Respiratory Depression Modulated by a Non-Opioid Agent," covering methods of treatment for the Company's novel proprietary agnostic respiratory stimulant product candidate, ENA-001. The granted patent has a term until January 2043 and builds upon the existing catalog of intellectual property for ENA-001, including composition of matter protection. "We are excited to have been granted this new patent for ENA-001 by the USPTO based on the innovative clinical activity of our scientific team," stated Joe Pergolizzi, M.D., Chief R&D Officer of Enalare Therapeutics. "Being able to fortify and extend the market exclusivity for a novel new chemical entity (NCE) like ENA-001 with this granted method of use patent helps ensure that we properly develop this one-of-a-kind agnostic respiratory stimulant with the potential to improve the lives of those impacted by several life-threatening conditions, including post-operative respiratory depression and community drug overdose, as well as a potential medical countermeasure in the case of mass-casualty events.""Being granted this new patent from the USPTO is recognition of ENA-001's therapeutic potential which is based on its novel and effective mechanism of action," stated Bob Raffa, Ph.D., Co-Founder and Head of Preclinical Development of Enalare Therapeutics. "We believe that ENA-001's differentiated approach to stimulating breathing by inhibiting Big Potassium (BK) ion channels in the carotid bodies, thus stimulating breathing across multiple etiologies of respiratory depression, regardless of its causality, offers the promise of becoming an important treatment option for patients experiencing a multitude of life-threatening conditions."This project has been funded in whole or in part with federal funds from the Department of Health and Human Services, Administration for Strategic Preparedness and Response, Biomedical Advanced Research and Development Authority, under contract number 75A50122C00072.The development of ENA-001 is also supported by the National Institute on Drug Abuse (NIDA) of the National Institutes of Health (NIH) under award number R44DA057133. The content of this document is the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health.About Enalare Therapeutics Inc.Enalare Therapeutics Inc. is a clinical-stage biopharmaceutical company dedicated to developing novel therapies for patients suffering from life-threatening critical care conditions and community-based health emergencies, including post-operative respiratory depression, community drug overdose, and apnea of prematurity. Enalare plans to initiate additional clinical studies for ENA-001 across multiple indications in the near term.About ENA-001Enalare's lead compound, ENA-001, is a one-of-a-kind new chemical entity (NCE) designed as an agnostic respiratory stimulant. The compound has a novel mechanism of action that affects ventilation via the peripheral chemoreceptor pathways in the carotid body. It utilizes the body's own ventilation control system to beneficially influence breathing and has been shown to be effective and well-tolerated in five human studies to date. With its novel mechanism of action and findings to date, it could potentially improve the lives of those impacted by several life-threatening conditions, including community drug overdose, post-operative respiratory depression, and apnea of prematurity. ENA-001 is an investigational compound and is not approved for use by the FDA.Forward-Looking Statement DisclaimerThis press release and any statements of representatives and partners of Enalare Therapeutics Inc. (the "Company") related thereto contain, or may contain, among other things, certain "forward-looking statements" within the meaning of the Private Securities Litigation Reform Act of 1995. Such forward-looking statements involve significant risks and uncertainties. Such statements may include, without limitation, statements with respect to the Company's plans, objectives, projections, expectations and intentions and other statements identified by words such as "projects," "may," "will," "could," "would," "should," "believes," "expects," "anticipates," "estimates," "intends," "plans," "potential" or similar expressions. Because forward-looking statements relate to the future, they are subject to inherent uncertainties, risks and changes in circumstances that are difficult to predict and many of which are outside of the Company's control. The Company's actual results may differ materially from those indicated in the forward-looking statements. Therefore, you should not rely on any of these forward-looking statements. Any forward-looking statements that the Company makes in this press release speak only as of the date of this press release. The Company assumes no obligation to update its forward-looking statements whether as a result of new information, future events or otherwise, after the date of this press release.###CONTACT:Morgan WagnerInvestor and Media Relations[email protected]SOURCE: Enalare Therapeutics Inc. View the original press release on newswire.com.Source: Enalare Therapeutics

10 Sep 2024

·www.newswire.com

Enalare Therapeutics Receives Additional Funding From BARDA to Further Advance the Development of Agnostic Respiratory Stimulant (ENA-001)

PRINCETON, N.J., September 10, 2024 (Newswire.com) - Enalare Therapeutics Inc., a clinical-stage biopharmaceutical company dedicated to developing novel compounds for the treatment of life-threatening critical care conditions and community health emergencies, today announced that it has received additional funding from the Biomedical Advanced Research and Development Authority (BARDA), part of the Administration for Strategic Preparedness and Response within the U.S. Department of Health and Human Services, to further advance the development of its lead compound, ENA-001. The supplementary funding of $4.97 million to the existing BARDA contract will be used to execute preclinical studies requested by the FDA in advance of Enalare proceeding forward with its intended phase 2 clinical study of ENA-001 for use in the hospital setting. This supplemental funding expands the 2022 contract, which now could provide up to $55.8 million to support the development of ENA-001. “We are very excited to announce this additional funding provided by BARDA and are grateful for their continued partnership and support of the development of ENA-001,” stated Joe Pergolizzi, MD, Chief R&D Officer of Enalare Therapeutics. “We believe ENA-001, with its novel mechanism of action as an agnostic respiratory stimulant, has the potential to improve the lives of those impacted by several life-threatening conditions, including post-operative respiratory depression (PORD) and community drug overdose, and as a potential medical countermeasure in the case of a mass-casualty event. We look forward to further strengthening our partnership with BARDA as we proceed forward with the development of ENA-001." This project has been funded in whole or in part with federal funds from the Biomedical Advanced Research and Development Authority (BARDA), part of the Administration for Strategic Preparedness and Response within the U.S. Department of Health and Human Services under contract 75A0122C00072. The development of ENA-001 is also supported by the National Institute on Drug Abuse (NIDA) of the National Institutes of Health (NIH) under award number R44DA057133. The content of this document is the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health. About Enalare Therapeutics Inc. Enalare Therapeutics Inc. is a clinical-stage biopharmaceutical company dedicated to developing novel therapies for patients suffering from life-threatening critical care conditions and community-based health emergencies, including post-operative respiratory depression, community drug overdose, and apnea of prematurity. Enalare plans to initiate additional clinical studies for ENA-001 across multiple indications in the near term. About ENA-001 Enalare's lead compound, ENA-001, is a one-of-a-kind new chemical entity (NCE) designed as an agnostic respiratory stimulant. The compound has a novel mechanism of action that affects ventilation via the peripheral chemoreceptor pathways in the carotid body. It utilizes the body's own ventilation control system to beneficially influence breathing and has been shown to be effective and well-tolerated in five human studies to date. With its novel mechanism of action and findings to date, it could potentially improve the lives of those impacted by several life-threatening conditions, including community drug overdose, post-operative respiratory depression, and apnea of prematurity. ENA-001 is an investigational compound and is not approved for use by the FDA. ### Source: Enalare Therapeutics Inc. BARDA Enalare Therapeutics Respiratory Depression Morgan Wagner Investor Relations mwagner@enalare.com Enalare Therapeutics is Granted a New Patent for ENA-001, Extending Its Exclusivity in the U.S. to 2043 6 days ago The New Patent Covers ENA-001 Methods of Treating Respiratory Depression Caused by Propofol, a Widely Used, Centrally Acting Anesthetic Enalare Receives FDA Clearance to Initiate the First Phase 1 Clinical Study of ENA-001 to Be Conducted in the United States 1 month ago Enalare Therapeutics Announces Publication of a Clinical Study Demonstrating the Effect of ENA-001 on Improving Propofol-Induced Depression of the Hypoxic Ventilatory Response 9 months ago

Phase 1Phase 2

100 Deals associated with Propofol

External Link

KEGG	Wiki	ATC	Drug Bank
D00549	Propofol	N01AX10	DB00818

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Anesthesia	US	Fresenius Kabi USA LLC	02 Oct 1989

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Sedation	Phase 1	CN	Shanghai Institute of Pharmaceutical Industry	03 Jan 2018
Sedation	Phase 1	CN	Beijing Sciecure Pharmaceutical Co., Ltd.	03 Jan 2018

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02820051 (CTgov)	Not Applicable	Sedation	102	Transcutaneous CO2 monitor+Midazolam+Lidocaine+nalbuphine (Midazolam)	lmdxaeaxse(nemkqatfts) = mlqgqlbkbn knjmqfojfn (pgxhjderfn, sjbtqriwob - mdlhigyooe) View more	-	02 Dec 2024
				Transcutaneous CO2 monitor+Propofol+Lidocaine+nalbuphine (Propofol)	lmdxaeaxse(nemkqatfts) = pvdaayfadr knjmqfojfn (pgxhjderfn, rttrthjrjp - wlnsnmggna) View more
UEGW2024	Not Applicable	-	-	Deep sedation with propofol	failgyqbyh(idgglinylb) = hxqaajjdqk iqpvvcibqq (hqbilydtxk ) View more	-	13 Oct 2024
UEGW	Not Applicable	-	-	Non-Anesthesiologist Administration of Propofol (NAAP)	igwzcvvkjp(wrwldivqwc) = bqcuvwyqdk snowwjmnmg (avopdjocrj ) View more	-	13 Oct 2024
				Anesthesiologist Administration of Propofol (AAP)	igwzcvvkjp(wrwldivqwc) = tmfbwtyknd snowwjmnmg (avopdjocrj ) View more
SFN2024	Not Applicable	-	-	Propofol anesthesia	fgznassjbi(adijnmygqb) = qdypvzixmk qpqzznsaxs (gwjeqekjxk, 3.14)	-	08 Oct 2024
NCT02697448 (CTgov)	Not Applicable	Atrial Fibrillation	135	propofol (Propofol)	hdamxocixb(ptadiwhbjw) = ctumkuswjc saqwewrpjn (zgwsvulbyf, kufrtgfdvk - gcpkaxoqna) View more	-	20 Aug 2024
				sevoflurane (Sevoflurane)	hdamxocixb(ptadiwhbjw) = jkilxvxmkb saqwewrpjn (zgwsvulbyf, nkeyizseoz - tunbbtiyod) View more
NCT02053766 (CTgov)	Not Applicable	Mitochondrial Diseases	19	Dexmedetomidine (Dexmedetomidine (Precedex®))	endvehipid(nldjiqujff) = ctsacdbgue toltrclqvh (rkbojaoskg, qwqevrbbzy - wiehxumnph) View more	-	17 Jul 2024
				Propofol (Propofol)	endvehipid(nldjiqujff) = bxpqenpabg toltrclqvh (rkbojaoskg, aegwdvfapn - wxqdmcneeb) View more
DDW2024	Not Applicable	Consciousness	-	Propofol (Patients with BIS <60)	lrazmxrutq(nwseaecdee) = 25% of patients with BIS<40, compared to 7.2% of patients without BIS<40; P=0.049 dzcimsvlub (eugnalyndd )	-	21 May 2024
				Propofol (Patients with BIS <40)
DDW2024	Not Applicable	Consciousness	-	Propofol (Patients with BIS <60)	xnsvvmjsdk(ibejzezdfj) = 25% of patients with BIS<40, compared to 7.2% of patients without BIS<40; P=0.049 xhwaonxglr (hsunuwwvwd )	-	21 May 2024
				Propofol (Patients with BIS <40)
DDW2024	Not Applicable	Consciousness	-	Propofol (Patients with BIS <60)	kgnpzdumie(qybsrxpjjq) = 25% of patients with BIS<40, compared to 7.2% of patients without BIS<40; P=0.049 axwgaemsys (iezhyknfpb )	-	21 May 2024
				Propofol (Patients with BIS <40)
DDW2024	Not Applicable	Consciousness	-	Propofol (Patients with BIS <60)	esypkoabqy(zzmefqjvfp) = 25% of patients with BIS<40, compared to 7.2% of patients without BIS<40; P=0.049 dxwiptaisv (uaqzgjdpvt )	-	21 May 2024
				Propofol (Patients with BIS <40)

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