Delving into the Latest Updates on Alfentanil Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Alfentanil hydrochloride (USP), Alfentanil sublingual, Alfentanyl

+ [7]

Target

Opioid receptors

Action

agonists

Mechanism

Opioid receptors agonists(Opioid receptors agonists)

Therapeutic Areas

Other Diseases

Active Indication

Anesthesia

Inactive Indication

Acute PainAnalgesia

Originator Organization

Akorn, Inc.

Active Organization

Rising Pharmaceuticals, Inc.

Yichang Humanwell Pharmaceuticals Co., Ltd.

Inactive Organization

Jiangsu Nhwa Pharmaceutical Co., Ltd.

Orexo AB

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (29 Dec 1986),

Anesthesia

RegulationOrphan Drug (United States), Priority Review (China)

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Structure/Sequence

Molecular FormulaC21H35ClN6O4

InChIKeyYYESXRRYBUERKF-UHFFFAOYSA-N

CAS Registry70879-28-6

Fentanyl analogs (fentalogs) share many structural and mass spectral similarities that make them difficult to differentiate and accurately identify without chromatog. data.In such situations, the expert algorithm for substance identification (EASI) provides superior classification relative to conventional approaches.Using a database of >57,000 replicate electron-ionization mass spectra of 76 fentalogs from ten laboratories, three challenging sets of isomers were studied in detail.To maximize limits of detection, only the 20 most abundant ions were considered.In each case, 50 % of the data from one laboratory served as the training set.On average, the mean absolute residuals between measured and modeled abundances of known positives were five times smaller using EASI than the consensus approach, which used the means of training sets as the exemplar spectra to which all query spectra were compared.With a conservative threshold of zero false positives, EASI identified isovalerylfentanyl from its two closest isomers with an accuracy of 96.7 %, which was ∼10 % better than the consensus approach.The associated pos. likelihood ratios increased from 366 for the consensus approach to more than 4,200 for EASI.When discriminating isovalerylfentanyl spectra from the other 72 fentalogs, EASI provided errorless results with a pos. likelihood ratio exceeding 50,000.For all 9 fentalogs, EASI outperformed the consensus approach and the use of Mahalanobis distance as a metric for identifying outliers.In the absence of retention time information, EASI improves confidence in drug identifications, enables inter-laboratory identifications, and reduces the need for acquiring concomitant spectra of standards

01 Jun 2025·FOOD CHEMISTRY

High-throughput screening of new psychoactive substances and related compounds in food by UHPLC-Q/Orbitrap

Article

Author: Huang, Xia ; Wan, Yuping ; Shi, Peiyu ; Wu, Wenlin ; Xiao, Quanwei ; Liu, Shiyao ; Guo, Tianrong ; Chen, Xiaoqi ; Zhang, Min ; Xia, Bing ; Zhou, Yan

Currently, there is concern about food products to which new psychoactive substances (NPS) have been added illegally. However, rapid, high-sensitivity, and high-throughput screening methods for such harmful substances have not been reported yet. In this study, a high-throughput non-targeted screening strategy was developed based on UHPLC-Q/Orbitrap. First, optimized pretreatment methods for typical high-risk matrices were established. Second, an accurate, efficient, and scalable high resolution mass spectrometry database containing 206 NPS and related compounds was constructed. The fragmentation pathways of three different types of fentanyl-related compounds were then systematically investigated to enhance compound identification. Additionally, a non-targeted screening strategy was developed using warning ions derived from 24 fentanyl-related compounds, streamlining the identification of NPS. This strategy was applied to 100 food samples with possible illegal additives and demonstrated its effectiveness. In summary, this study provides robust technical support for regulatory authorities in combating the illegal addition of food products.

01 May 2025·PHYTOMEDICINE

Integrating untargeted/targeted metabolomics and network pharmacology association analysis to study the mechanism of safflower regulating C18:0 sphingolipid metabolism to treat acute myocardial ischemia

Article

Author: Chen, Jia ; Wei, Feng ; Jia, Zhixin ; Zhang, Ping ; Fang, Cong ; Liu, Mengjiao ; Cheng, Xianlong ; Pan, Mingxia ; Yan, Hua

BACKGROUND:

Safflower extract (SE) has been reported to treat acute myocardial ischemia (AMI); however, its underlying mechanism remains unclear.

PURPOSE:

To investigate the ameliorative effects of SE on rats with AMI and the underlying mechanism.

METHODS:

UPLC-Q-TOF-MS/MS method was used to analyze the drug-derived components in the serum of rats following SE administration. We treated the ISO-induced rat model of AMI with different doses. Echocardiography and histopathology (HE staining) were used to evaluate the effect, alongside biochemical parameters. SE medicinal serum (SEMS) was used to assess its protective effect on H9C2 cells against hypoxic reoxygenation injury in vitro. We explored the mechanism of SE in improving AMI through non-targeted metabolomics combined with network pharmacological analysis based on in vivo components, and further integrated with targeted sphingolipomics. RT-qPCR was used to evaluate the gene expression levels of the key enzymes involved in ceramide synthesis (CERS1 and CERS4).

RESULTS:

Nineteen compounds were identified following oral administration of SE. Echocardiography showed that different doses of SE significantly improved cardiac function in AMI rats. The serum levels of CK, HBDH, AST, LDH, and SOD were significantly reduced in AMI rats. HE staining results showed that SE significantly improved pathological injury in AMI rats. In vitro experiments results showed that SEMS protects against OGD/R injury in H9C2 cells. Non-targeted metabolomics and network pharmacology results indicated that SE regulates glycosphingolipid and glycerophospholipid metabolism to improve acute myocardial ischemic injury. Targeted sphingolipomics have shown that SE had significant regulatory effects on 18:0 acyl-chain ceramides, dihydroceramides, 1-phosphorylated ceramides, glycosylated ceramides, Sph and S1P. RT-qPCR results showed that SE significantly down-regulates the expression of mCERS4.

CONCLUSIONS:

SE significantly improves AMI in rats, with the mechanism related to the regulation of CERS4 and then the modulation of C18:0 sphingolipid metabolism.

2

News (Medical) associated with Alfentanil Hydrochloride

14 Mar 2025

·www.echemi.com

5 Key Updates on China's Fentanyl Control Amid US Tariffs

On February 1st, the United States announced a 10% tariff on products imported from China, citing concerns over the fentanyl crisis. In response, a spokesperson from the Ministry of Public Security emphasized that China maintains one of the strictest drug control policies in the world. As a signatory to the three UN drug control conventions, China has consistently upheld its international obligations and actively collaborates with countries, including the US, on drug enforcement efforts. In 2019, China took a humanitarian step by becoming the first country to classify all fentanyl-related substances under stringent controls, responding to US requests. Since this classification, China has not received reports of these substances being seized in the US. On March 12th, the National Medical Products Administration (NMPA) shared insights regarding China's management of fentanyl substances through a recently released white paper. The spokesperson addressed concerns about the production and export of fentanyl-related pharmaceuticals. Currently, four fentanyl-related drugs are approved for clinical use in China: fentanyl, sufentanil, remifentanil, and alfentanil. Three companies have been authorized to produce raw materials, while five are permitted to manufacture formulations. In 2024, China produced 100 kilograms of fentanyl raw materials, primarily for domestic medical use and export, with only 12.3 kilograms exported to countries like South Korea, Vietnam, and the Philippines. Notably, China has never exported fentanyl products to North America. All fentanyl-related drugs in China are classified as controlled narcotics, subjected to stringent regulations. The production and distribution of these drugs are closely monitored, with specific companies designated for manufacturing and fixed sales channels established. Export controls require permits, and international verification ensures the legality of trade before issuing export licenses. The NMPA will continue to enhance the supervision of fentanyl-related drug production and strictly regulate exports to prevent illegal channels and misuse, ensuring that medical needs are met responsibly.

Drug Approval

21 Jan 2025

·www.echemi.com

Humanwell Healthcare Secures Major Investment: A New Era Begins with Strategic Backing

After a three-month hiatus, leading domestic anesthetics producer Humanwell Healthcare has officially been "acquired" by a state-backed entity. On January 15, the company announced that it had signed a restructuring investment agreement with Zhaoshang Innovation Technology Group Co., Ltd. and its management team. This collaboration involves an investment of ¥11.8 billion, positioning Zhaoshang Innovation as the new controlling shareholder, with a 23.70% stake in Humanwell Healthcare. The restructuring investment will be executed in two phases. The first phase, covering 60% of the investment, will be paid upon the approval of the restructuring plan by the Wuhan Intermediate People’s Court. The remaining 40% will be paid after the completion of stock and voting rights transfers. Once this restructuring plan is finalized, Humanwell Healthcare will officially transition to state-owned control, a move that has significantly boosted its stock price, reaching ¥23.6 per share and a market capitalization of ¥38.52 billion. A Shift in Leadership: Hope for the "Anesthetic King" Founded in 1993, Humanwell Healthcare was once the dominant force in the anesthetic drugs sector. However, it has faced unprecedented challenges due to its former major shareholder, Dandai Technology, being mired in a debt crisis. Previously, six potential restructuring investors had passed the initial review, including three state-owned enterprises and three large local state-owned enterprises. Dandai Technology’s 23.7% stake in Humanwell Healthcare is currently frozen due to judicial actions. The entry of Zhaoshang Innovation brings a glimmer of hope, with the investment structured in three parts: Direct acquisition of 6% of Humanwell Healthcare’s shares. Indirect acquisition of another 6% through a new limited partnership in the Donghu New Technology Development Zone, with Zhaoshang Innovation as the general partner. Trust plan acquiring 11.70% of shares, with all voting rights delegated to Zhaoshang Innovation. Zhaoshang Innovation is controlled by China Merchants Group, a significant state-owned enterprise headquartered in Hong Kong. In 2023, China Merchants Group reported revenues of ¥924.4 billion and a net profit of ¥191.1 billion, showcasing its robust financial standing. Strategic Investment Amid Market Challenges Zhaoshang Innovation's substantial investment indicates its strategic interest in Humanwell Healthcare's industry-leading position in the pharmaceutical sector. Humanwell Healthcare is one of the few companies capable of producing a full range of fentanyl products and has established a strong foothold in various segments, including anesthetics and steroid hormones. According to the latest data, Humanwell Healthcare holds a 25.9% market share in the anesthetics market, making it the leading player. Its products, including alfentanil and hydromorphone, have a 100% market share, illustrating its dominance. In the past five years, Humanwell Healthcare has invested ¥4.6 billion in research and development, reflecting a commitment to innovation. In 2023, R&D expenses surpassed ¥1 billion, with a 9.2% increase in the first three quarters of 2024. The company has received approval for 1 traditional Chinese medicine and 17 chemical drug products, indicating a robust pipeline for future growth. Despite these positive developments, challenges remain. The competitive landscape is fierce, and the company must ensure that its R&D investments yield proportional returns. The support from Zhaoshang Innovation may provide the necessary impetus for Humanwell Healthcare to navigate these challenges successfully and emerge stronger. With Zhaoshang Innovation taking a controlling stake, Humanwell Healthcare's ownership issue has reached a significant resolution. This strategic investment from a state-owned entity sends positive signals to the market. However, the company still faces challenges related to market competition and R&D efficiency. Observers will be keen to see if Humanwell Healthcare can leverage this new partnership to overcome its obstacles and achieve a successful turnaround.

AcquisitionDrug Approval

100 Deals associated with Alfentanil Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D00835	Alfentanil Hydrochloride	N01AH02	DB00802

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Anesthesia	United States	Rising Pharmaceuticals, Inc.	29 Dec 1986

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Analgesia	Phase 3	China	Jiangsu Nhwa Pharmaceutical Co., Ltd.	06 Jun 2018
Acute Pain	Phase 3	Czechia	Orexo AB	08 Oct 2012

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ChiCTR2200062034 (Pubmed \| BMC Anesthesiol)	Phase 1	-	96	Alfentanil 20 µg/kg	tpihqmmcon(rolutbjjee) = xdqmlkcgkt alufrvzjnh (hmexkprebk ) View more	Positive	13 Aug 2024
				Alfentanil 25 µg/kg	qigrbukiyc(plvxpixaao) = aobsagkwmh vmlnwwvowh (kejltbtkqw )
NCT03359395 (CTgov)	Phase 4	Hypotension	100	Alfentanil (Alfentanil)	qiusufewgf(lhanbpqidy) = lqqqtyddzn ltmnrhtlik (seebemdloo, 36.968) View more	-	08 Jul 2021
				Placebos (Placebo)	qiusufewgf(lhanbpqidy) = fngidiaxqb ltmnrhtlik (seebemdloo, 33.50864) View more
NCT01008059 (CTgov)	Not Applicable	-	6	Alfentanil	qxypekxcgm(cxuaesydjp) = cikdsybthb ptwvezrkgy (jpedgfwdtg, 15) View more	-	17 May 2019
NCT01094574 (CTgov)	Not Applicable	Pain \| Inflammation	10	Alfentanil (Alfentanil)	ehkanakamq(tzpfnsvcfl) = ippydvjjwa nrvwqqdznv (zmwjhcxwlo, 0.74) View more	-	24 Feb 2017
				Propranolol (Propranolol)	ehkanakamq(tzpfnsvcfl) = dbypawnrzs nrvwqqdznv (zmwjhcxwlo, 0.26) View more
NCT00997126 (CTgov)	Phase 4	Sedation	126	propofol (Propofol)	ywaqybfuri = idwnalekxr uzxeknawvb (arkhjggqua, hlnpcaeazc - fruhmturji) View more	-	27 Jan 2017
				Alfentanil (Alfentanil)	ywaqybfuri = awnhtvtwvp uzxeknawvb (arkhjggqua, kmrzbpddfb - sqbjnehjif) View more
NCT00672438 (CTgov)	Not Applicable	Pain	242	Alfentanil	djzdhcssqz(dltxwkgyus) = mfpwhlqlmk tpqogamqly (mzoomxnxzk, ixakhjjwmh - kncfwnsxfw) View more	-	21 Jul 2016
NCT01470170 (CTgov)	Phase 4	Hypoxia	173	Targeted controlled infusion+propofol+Normal saline+Alfentanil (Group1)	uxtigqnmyb(mgxyzuopgj) = xmjyfkixqn ahumuuaicf (lmfadqwpmc, 0.4) View more	-	13 Aug 2015
				Targeted controlled infusion+propofol+Normal saline+Alfentanil (Group 3)	uxtigqnmyb(mgxyzuopgj) = ylsstdvybz ahumuuaicf (lmfadqwpmc, 0.4) View more
NCT00997113 (CTgov)	Phase 4	Sedation	20	propofol (Propofol)	jbqrckxwcd(ponbbmgsto) = puxwywmlvz vkimtjaoei (rzlzdeeiml, nsedtnqzln - ejjscwymst) View more	-	25 Sep 2014
				propofol+alfentanil (Propofol/Alfentanil)	jbqrckxwcd(ponbbmgsto) = vchzyeuqdo vkimtjaoei (rzlzdeeiml, nnmtihnfea - taedzotdos) View more
Pubmed \| Clin J Pain	Not Applicable	Pain	-	Alfentanil 15 mcg/kg	afnrzyvpkf(dwsioudjhr) = zgxivlzeig tmjxaqzpmc (zkcqnvkxov, ±26.5)	-	01 Jan 2014
NCT00991809 (0813, CTgov)	Not Applicable	Hyperalgesia	22	Alfentanil (Alfentanil)	ymvmlldwzd(okdsejmybb) = fpsvinkwvj uiwpzihzmr (kxvahnufyd, ujumvkwxym - vdjnkcgesu) View more	-	14 Oct 2013
				Diphenhydramine (Diphenhydramine)	ymvmlldwzd(okdsejmybb) = nexvanahkk uiwpzihzmr (kxvahnufyd, qmomlcbnku - xtrtgjvdbn) View more