Delving into the Latest Updates on Tasimelteon with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

N-{[(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl}propanamide, Tasimelteon (USAN/INN)

+ [4]

Target

Melatonin receptor

Mechanism

Melatonin receptor agonists

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

Sleep Initiation and Maintenance DisordersSleep Wake DisordersJet Lag Syndrome+ [3]

Inactive Indication

Depressive Disorder, MajorLiver DiseasesPervasive child development disorders+ [3]

Originator Organization

Vanda Pharmaceuticals, Inc.

Active Organization

Vanda Pharmaceuticals Netherlands BV

Vanda Pharmaceuticals, Inc.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

US (31 Jan 2014),

Sleep Wake Disorders

RegulationOrphan Drug (EU), Priority Review (US)

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Structure

Molecular FormulaC15H19NO2

InChIKeyPTOIAAWZLUQTIO-GXFFZTMASA-N

CAS Registry609799-22-6

To assess the effects of a daily single oral dose of 20 mg tasimelteon compared to baseline on events of dream enactment on patients with REM Behavior Disorder, as measured by a daily log.
To assess the effects of 20 mg tasimelteon compared to baseline on insomnia= symptoms, as measured by validated questionnaires (Insomnia Severity Index [ISI], Pittsburgh Sleep Quality Inventory [PSQI], Epworth Sleepiness Scale [ESS], Clinical Global Impression of Change Scale (CGI-C), Patient Global Impression of Change Scale (PGI-C)) as well as rest/activity pattern from actigraphy.
To assess the effects of 20 mg tasimelteon on patients who have a reduced or aberrant melatonin secretion compared to normal secretion by measuring salivary DLMO at baseline and correlating with the degree of change in RBD symptoms by end of the study.
To assess for any role a patient's unique genome may play in their response to tasimelteon; obtained via whole genome sequencing.
To assess the safety and tolerability of a daily single oral dose of 20 mg tasimelteon.

Start Date30 Sep 2023

Sponsor / Collaborator

The Brigham & Women's Hospital, Inc.

[+1]

NCT05572281 / CompletedPhase 1

An Open-Label, Two-Period, Randomized, Single Oral Dose, Crossover Study to Evaluate the Bioequivalence of Tasimelteon Capsule Formulation Relative to Tasimelteon Liquid Suspension Formulation in Healthy Volunteers

This is a single center, two-period, randomized study to evaluate the bioequivalence of a single dose of tasimelteon capsule formulation relative to a single dose of liquid suspension formation in healthy volunteers.

Start Date18 May 2022

Sponsor / Collaborator

Vanda Pharmaceuticals, Inc.

NCT05361707 / RecruitingPhase 3

A Study to Evaluate the Efficacy and Safety of Tasimelteon in Treating Sleep Disturbances in Individuals With Autism Spectrum Disorder

This is a multicenter, open-label study to evaluate the efficacy and safety of a daily single oral dose of tasimelteon in treating sleep disturbances in pediatric and adult participants with ASD.

Start Date28 Jul 2021

Sponsor / Collaborator

Vanda Pharmaceuticals, Inc.

100 Clinical Results associated with Tasimelteon

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100 Translational Medicine associated with Tasimelteon

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100 Patents (Medical) associated with Tasimelteon

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125

Literatures (Medical) associated with Tasimelteon

01 Nov 2024·Science of The Total Environment

Effects of low-molecular-weight organic acids on the transport of polystyrene nanoplastics: An insight at the structure of organic acids

Article

Author: Wei, Xuan ; Chen, Feiyu ; Gong, Yi ; Lu, Taotao ; Chen, Dong

Plastic nanoparticles are extensively used in various products, leading to inevitable pollution in soil. Understanding their transport in soils where various organic substances exist is crucial. This study examined the impact of low-molecular-weight organic acids (LMWOAs) on the transport of polystyrene nanoplastics (PS-NPs) through saturated quartz sand. The experiments involved three dibasic acids-malonic acid (MA₁), malic acid (MA₂) and tartaric acid (TA) - and four monobasic acids- formic acid (FA), acetic acid (AA), propanoic acid (PA) and glycolic acid (GA) -under different pH levels (4.0, 5.5, 7.0) and in the presence of cations (Na⁺, Ca²⁺). The results demonstrated that in the presence of Na⁺, dibasic acids significantly enhanced PS-NPs transport, with TA being the most effective, followed by MA₂ and MA₁. This enhancement is attributed to the adsorption of LMWOAs onto the nanoparticles and sand, creating a more negative ζ-potential, which increases the electrostatic repulsion and decreases the PS-NPs deposition, thereby facilitating the transport. Applying the Derjaguin-Landau-Verwey-Overbeek theory, higher pH levels increased the energy barrier and secondary energy minimum, decreasing PS-NPs deposition. Moreover, dibasic acids significantly enhanced the hydrophilicity of PS-NPs. Conversely, monobasic acids, except for GA, slightly reduced the hydrophilicity of PS-NPs, as indicated by a small increase in the water contact angle, hereby minimally affecting PS-NPs transport. As for GA, although it is a monobasic acid, the additional -OH group in its molecular structure promoted PS-NPs transport, similar to dibasic acids. For example, GA also significantly enhanced the hydrophilicity of PS-NPs. In the presence of Ca²⁺, the enhancement of PS-NPs transport by LMWOAs was comparable to that with Na⁺, primarily due to the complex-forming and bridging effects of Ca²⁺ with the organic acids and PS-NPs. These findings provide important insights into predicting and analyzing the transport behaviors of PS-NPs.

01 Aug 2024·Journal of Pineal Research

Relationship Between Melatonin Receptor Agonists and Parkinson's Disease

Article

Author: Noguchi, Yoshihiro ; Yoshimura, Tomoaki ; Aizawa, Haruka ; Masuda, Rikuto

AbstractParkinson's disease affects millions of people worldwide, and without significant progress in disease prevention and treatment, its incidence and prevalence could increase by more than 30% by 2030. Researchers have focused on targeting sleep and the circadian system as a novel treatment strategy for Parkinson's disease. This study investigated the association between melatonin receptor agonists and Parkinson's disease, using the Food and Drug Administration (FDA) Adverse Events Reporting System (FAERS). The target drugs were melatonin receptor agonists including ramelteon, tasimelteon, and agomelatine. Parkinson's disease cases were defined according to the Medical Dictionary for Regulatory Activities (MedDRA) 25.0; Standardized MedDRA Query (SMQ) using both the “narrow” and “broad” preferred terms (PTs) associated with Parkinson's disease. The association between melatonin receptor agonists (ramelteon, tasimelteon, and agomelatine) and Parkinson's disease was evaluated by the reporting odds ratio. Upon analyzing the data from all patients registered in the FAERS, ramelteon (ROR: 0.66, 95% confidence interval [95% CI]: 0.51–0.84) and tasimelteon (ROR: 0.49, 95% CI: 0.38–0.62) showed negative correlations with Parkinson's disease. Conversely, only agomelatine was positively correlated with Parkinson's disease (ROR: 2.63, 95% CI: 2.04–3.40). These results suggest that among the melatonin receptor agonists, ramelteon and tasimelteon are negatively correlated with Parkinson's disease. In contrast, agomelatine was shown to be positively correlated with Parkinson's disease. These results should be used in research to develop drugs for the treatment of Parkinson's disease, fully considering the limitations of the spontaneous reporting system.

01 Apr 2024·Sleep Medicine

Improvement in non-24-h sleep-wake rhythm disorder in a sighted individual treated with a melatonin receptor agonist

Article

Author: Davis, Eric M ; Connolly, Patrick J ; Quigg, Mark

Non-24-hour sleep-wake rhythm disorder (N24SWD) typically presents in patients with visual impairments that disrupt the ability to entrain to the 24 hour solar cycle. We discuss a 43 year old sighted man who presented with periodic daytime hypersomnia and nighttime insomnia, occasionally leading to <3 hours of sleep per day. Previous polysomnography showed an apnea hypopnea index of 6.2 events per hour. A sleep log of 3 months showed irregular time of sleep onset, and an average of 3 hours of sleep per day. Wrist actigraphy confirmed N24SWD. A trial of tasimelteon 20 mg/day resulting in improved daytime hypersomnia (pre-Epworth Sleepiness Scale (ESS) = 21/24, post-ESS = 5/24; a score of > 10/24 is considered sleepy). Follow-up actigraphy showed marked resolution of phase delay with an average of five hours of sleep. The case demonstrates that tasimelteon is a possible treatment for N24SWD in sighted individuals.

44

News (Medical) associated with Tasimelteon

01 Jul 2024

·www.prnewswire.com

Federal Court Allows Vanda's HETLIOZ® Patent Lawsuit to Proceed against Teva and Apotex

WASHINGTON, July 1, 2024 /PRNewswire/ -- Vanda Pharmaceuticals Inc. (Vanda) (Nasdaq: VNDA) today announced that the U.S. District Court for the District of Delaware (the "Court") denied the motions for judgment on the pleadings that were filed by Teva Pharmaceuticals USA, Inc. ("Teva") and Apotex Inc. and Apotex Corp. ("Apotex") and ordered that Vanda's HETLIOZ® patent lawsuit may proceed. Vanda brought this suit in December 2022, alleging patent infringement against Teva and Apotex (the "Defendants"). The Defendants moved for judgment on the pleadings in April 2023. On June 27, 2024, the Court denied the motions. The Court concluded that the issues of patentability were not the same as those resolved in prior patent-infringement litigation between the parties. It further concluded that the Defendants raised issues that require claim construction and fact development before the Court can resolve the case. Vanda intends to proceed with discovery in the case to continue pursuing its claims. Vanda will request relief from the Court that includes an order requiring the Defendants to discontinue marketing their generic versions of HETLIOZ® until the expiration of the patent-in-suit and enjoining them from the commercial manufacture, use, import, offer for sale and/or sale of these products. About Vanda Pharmaceuticals Inc. Vanda is a leading global biopharmaceutical company focused on the development and commercialization of innovative therapies to address high unmet medical needs and improve the lives of patients. For more on Vanda Pharmaceuticals Inc., please visit and follow us on X @vandapharma. About HETLIOZ® For full U.S. Prescribing Information for HETLIOZ®, including indication and Important Safety Information, visit . CAUTIONARY NOTE REGARDING FORWARD-LOOKING STATEMENTS Various statements in this press release, including, but not limited to statements regarding Vanda's intentions to proceed with discovery in pursuit of its claims and to request relief from the Court, are "forward-looking statements" under the securities laws. All statements other than statements of historical fact are statements that could be deemed forward-looking statements. Forward-looking statements are based upon current expectations and assumptions that involve risks, changes in circumstances and uncertainties. Important factors that could cause actual results to differ materially from those reflected in Vanda's forward-looking statements include, among others, the results of Vanda's discovery and the Court's willingness to grant Vanda the relief that it seeks. Therefore, no assurance can be given that the results or developments anticipated by Vanda will be realized or, even if substantially realized, that they will have the expected consequences to, or effects on, Vanda. Forward-looking statements in this press release should be evaluated together with the various risks and uncertainties that affect Vanda's business and market, particularly those identified in the "Cautionary Note Regarding Forward-Looking Statements", "Risk Factors" and "Management's Discussion and Analysis of Financial Condition and Results of Operations" sections of Vanda's most recent Annual Report on Form 10-K, as updated by Vanda's subsequent Quarterly Reports on Form 10-Q, Current Reports on Form 8-K and other filings with the U.S. Securities and Exchange Commission, which are available at . All written and verbal forward-looking statements attributable to Vanda or any person acting on its behalf are expressly qualified in their entirety by the cautionary statements contained or referred to herein. Vanda cautions investors not to rely too heavily on the forward-looking statements Vanda makes or that are made on its behalf. The information in this press release is provided only as of the date of this press release, and Vanda undertakes no obligation, and specifically declines any obligation, to update or revise publicly any forward-looking statements, whether as a result of new information, future events or otherwise, except as required by law. Corporate Contact: Kevin Moran Senior Vice President, Chief Financial Officer and Treasurer Vanda Pharmaceuticals Inc. 202-734-3400 [email protected] Jim Golden / Jack Kelleher / Dan Moore Collected Strategies [email protected] SOURCE Vanda Pharmaceuticals Inc.

Patent Infringement

20 Jun 2024

·www.fiercepharma.com

Vanda rejects buyout offers, pans 'opportunistic attempts' at securing its shares at a discount

Vanda has rejected multiple buyout proposals and is proceeding with its prior plans, the company said in a statement. A series of increasing buyout offers has failed to convince Vanda's board of directors that the company should sell itself. After receiving "unsolicited" buyout proposals from Michigan-based CDMO Future Pak and U.K. drugmaker Cycle Pharmaceuticals, Vanda's board concluded that both offers "substantially undervalue" the company. Vanda has rejected the proposals, the company said in a June 19 press release. Starting in February, Future Pak began submitting a series of proposals to acquire Vanda. In April, Future Pak revealed that it was willing to buy Vanda for $7.25 to $7.75 per share. The following month, Future Pak boosted its offer by floating contingent value rights worth up to $260 million tied to specific future commercial and regulatory accomplishments by Vanda. Early this month, Cycle Pharma got involved with a buyout offer of $8 per share, or $466 million in total. At the time, Vanda said it would "carefully review and evaluate the indication of interest" in the proposal. Now, Vanda is turning back both offers in favor of proceeding with its own plan. "The Vanda board again evaluated all aspects of Vanda's business against the unsolicited proposals and determined that the proposals are opportunistic attempts to purchase the company's shares at a discount to Vanda's intrinsic value," Vanda said in a statement. "The board's prior analysis of the company's clinical development pipeline, expanding commercial presence and significant cash balance remains unchanged." Vanda said its revenue base, cash position and efficient operations position the company "for significant long-term growth and value creation far in excess of the" other firms' offers. Vanda's share price has enjoyed a multi-month rally since a low of $3.47 in early February, rising to $6.50 last week. With the news that Vanda rejected the proposals, shares traded down by about 8% early Thursday. Vanda generated $192 million in 2023, a 24% decrease from the prior year as sleep disorder drug Hetlioz posted sharply lower sales thanks to U.S. generic competition. Seeking to regroup for a new phase of growth, Vanda recently acquired Ponvory, a former Johnson & Johnson multiple sclerosis drug, for $100 million. And its schizophrenia stalwart Fanapt won an expanded label to treat bipolar I disorder.

Acquisition

07 Jun 2024

·www.biospace.com

Vanda Gets $466M Unsolicited Offer from Cycle Amid Ongoing Row with FDA

Pictured: Boardroom overlooking a city/iStock, ismagilov Vanda Pharmaceuticals on Thursday confirmed that it has received an unsolicited and non-binding takeover offer from Cycle Pharmaceuticals for $8 per share, a price Vanda’s stock has not traded at since January 2023. Cycle in a separate announcement noted that its per-share offer represents a 63% premium to Vanda’s closing price on May 23, 2024, the day before Cycle submitted its takeover proposal, and a 58% premium to the biotech’s closing share price on Wednesday. The deal’s total cash consideration is $466 million. According to Cycle, its offer “delivers immediate, compelling and certain cash value for Vanda shareholders, with a highly attractive premium,” noting that the deal would also benefit patients given Cycle’s “proven commercial strategy in the U.S., a strong distribution footprint and an established track record of delivering medicines and individualized support to patients.” Cycle’s offer also trumps Future Pak’s revised takeover bid. Filed in May 2024, Future Pak’s new proposal was valued at $7.25 to $7.75 per share plus certain contingent value rights (CVR). Vanda previously turned down an initial proposal from Future Pak, which offered a similar per-share price range without the CVR. Vanda said on Thursday that its board of directors will “carefully review and determine” its course of action regarding Cycle’s offer. The company is staying mum on the further details of the deal and its interest in the offer, but has said that shareholders currently have no need to take any action. Cycle’s takeover offer comes as Vanda is engaged in a regulatory row with the FDA. In February 2024, the agency denied to approve Vanda’s supplemental New Drug Application (sNDA), which was seeking to use its oral drug Hetlioz (tasimelteon) to treat insomnia as characterized by difficulty with sleep initiation. At the time, Vanda said that “no deficiencies were disclosed by the FDA in the notification.” The biotech slammed the regulator’s rejection, saying that it “believes that the timing of the FDA’s communication is part of an ongoing violation of the Federal Food Drug, and Cosmetic Act (FDCA),” which requires the regulator to “either approval a new drug application or provide an opportunity for a hearing within 180 days after the filing of an application.” Vanda filed its sNDA on May 4, 2023, which means the FDA’s FDCA-mandated deadline was on October 31, 2023. “The FDA has not complied with the statute and has not timely approved the application or provided an opportunity for a hearing within the statutorily prescribed timeframe,” according to the biotech. In a rare move, the FDA on Friday released documentation detailing its reasons for rejecting Hetlioz and giving Vanda the option to seek a hearing. According to the regulator, the biotech’s application “does not provide substantial evidence of effectiveness for tasimelteon and does not demonstrate that the drug is safe for the treatment of insomnia.” Tristan Manalac is an independent science writer based in Metro Manila, Philippines. Reach out to him on LinkedIn or email him at tristan@tristanmanalac.com or tristan.manalac@biospace.com.

AcquisitionDrug Approval

100 Deals associated with Tasimelteon

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External Link

KEGG	Wiki	ATC	Drug Bank
D09388	Tasimelteon	N05CH03	DB09071

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Sleep Initiation and Maintenance Disorders	US	Vanda Pharmaceuticals, Inc.	01 Dec 2020
Sleep Wake Disorders	US	Vanda Pharmaceuticals, Inc.	31 Jan 2014

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Jet Lag Syndrome	NDA/BLA	US	Vanda Pharmaceuticals, Inc.	-
Pervasive child development disorders	Phase 3	US	Vanda Pharmaceuticals, Inc.	16 Sep 2021
Autism Spectrum Disorder	Phase 3	US	Vanda Pharmaceuticals, Inc.	28 Jul 2021
Sleep Deprivation	Phase 3	US	Vanda Pharmaceuticals, Inc.	01 Sep 2015
Smith-Magenis Syndrome	Phase 3	US	Vanda Pharmaceuticals, Inc.	01 Sep 2015
Renal Insufficiency	Phase 3	US	Vanda Pharmaceuticals, Inc.	01 Feb 2012
Depressive Disorder, Major	Phase 3	US	Vanda Pharmaceuticals, Inc.	01 Sep 2011
Liver Diseases	Phase 3	US	Vanda Pharmaceuticals, Inc.	01 Jan 2011
Sleep Disorders, Circadian Rhythm	Phase 3	DE	Vanda Pharmaceuticals, Inc.	01 Aug 2010
Sleep Disorders, Circadian Rhythm	Phase 3	US	Vanda Pharmaceuticals, Inc.	01 Aug 2010

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03373201 (CTgov)	Phase 3	Jet Lag Syndrome	320	Placebo (Placebo)	noocuashda(wifeyayehl) = opuisoxwlm krkxmyxabj (vbumjdlqrr, ywuqstwzav - bhztymarzi) View more	-	15 Sep 2023
				Tasimelteon (Tasimelteon)	noocuashda(wifeyayehl) = fgxiphifbo krkxmyxabj (vbumjdlqrr, ysqfwdjsuj - sjncnomvmk) View more
NCT03291041 (JET, Pubmed) Manual	Phase 2	Jet Lag Syndrome	25	tasimelteon	tglkbbcxui(ndcmxibyks): difference = 131	Positive	15 Sep 2022
				Placebo
NCT03291041 (JET, CTgov)	Phase 2	Jet Lag Syndrome	25	Tasimelteon (Tasimelteon)	ptqjlzedlm(psbigngjve) = obxulhopib dtkvrbqjvr (edarbrddgd, dbnxkbitun - qowqsayxso) View more	-	03 Nov 2021
				Placebo (Placebo)	ptqjlzedlm(psbigngjve) = zufvauxwym dtkvrbqjvr (edarbrddgd, bvycacwwyv - xuaoozubmo) View more
JET8 (WSC2019)	Not Applicable	-	318	Tasimelteon	sixozurdyj(kuxccthhll) = slgijsxeub ynsngqigeq (ljxrkgwrfq )	Positive	20 Sep 2019
Magellan study (tasimelteon in MDD study) (WSC2017)	Not Applicable	Depressive Disorder, Major	507	Tasimelteon 20 mg	(llxptwhqmz) = svamdshutk dcvfqvkwso (wxizolpzhj ) View more	Positive	07 Oct 2017
				Placebo	(llxptwhqmz) = dlwnqmjzsr dcvfqvkwso (wxizolpzhj ) View more
NCT01163032 (SET, Pubmed \| Lancet) Manual	Phase 3	Sleep Disorders, Circadian Rhythm	84	tasimelteon	svqwvkvdmr(hdwuefhbsx) = vdngogkznf yxjihqqbyo (hhvzwmumyo ) View more	Positive	31 Oct 2015
				Placebo	svqwvkvdmr(hdwuefhbsx) = itkyekucxe yxjihqqbyo (hhvzwmumyo ) View more
NCT01428661 (MAGELLAN, CTgov)	Phase 2/3	Depressive Disorder, Major	507	tasimelteon (Tasimelteon)	iemfppngbk(fhapmqeqsa) = jdmuznwany mjqejumqol (vrtydtsutf, vksdlszxgk - hjctwxnjzy) View more	-	19 Jun 2015
				placebo (Placebo)	iemfppngbk(fhapmqeqsa) = ygqncwtexx mjqejumqol (vrtydtsutf, sqlbxsxgnm - yxlcywebtf) View more
NCT01163032 (SET, CTgov)	Phase 3	Sleep Disorders, Circadian Rhythm	136	tasimelteon (Tasimelteon (Randomized))	pznjhrnvmg(vjhfztcoas) = vttgnorstj zsaxojepqf (dcsuqvzamx, fhmmtuifmc - anloxbqmxf) View more	-	16 Oct 2014
				Placebo (Placebo (Randomized))	pznjhrnvmg(vjhfztcoas) = oncaqyayva zsaxojepqf (dcsuqvzamx, azzooexllq - xjrmtuiylj) View more
NCT00291187 (CTgov)	Phase 3	Sleep Initiation and Maintenance Disorders	411	Placebo	mumscgtmfw(nshdtsuacx) = uvgsvuwzbh guyrjdijfv (bdhxkvbzlp, vwqeqxoagm - oyiapzsvnu) View more	-	15 Oct 2014
NCT01430754 (RESET, CTgov)	Phase 3	Sleep Disorders, Circadian Rhythm	20	tasimelteon (Tasimelteon)	mevhlapcih(rqhsbgcpum) = auqvpfqfmq xvjnsvulgc (qjtljpzyou, igrmhnllka - miepixfimm) View more	-	10 Oct 2014
				Placebo (Placebo)	mevhlapcih(rqhsbgcpum) = wntzycabss xvjnsvulgc (qjtljpzyou, pwppsnlmhg - bshldkgaqk) View more