Delving into the Latest Updates on Bexarotene with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

4-[1-(3,5,5,8,8-pentamethyltetralin-2-yl)ethenyl]benzoic acid, 4-[1-(5,6,7,8,-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphtalenyl)ethenyl]benzoic acid, Bexarotene (JAN/USAN/INN)

+ [21]

Target

RXRs

Action

agonists, inhibitors

Mechanism

RXRs agonists(Retinoid X receptor agonists), Protein synthesis inhibitors

Therapeutic Areas

NeoplasmsImmune System DiseasesHemic and Lymphatic Diseases+ [5]

Active Indication

Cutaneous T-Cell LymphomaCushing SyndromeEsophageal Squamous Cell Carcinoma+ [2]

Inactive Indication

Advanced breast cancerAdvanced Lung AdenocarcinomaAdvanced Lung Non-Small Cell Carcinoma+ [9]

Originator Organization

Ligand Pharmaceuticals, Inc.

Active Organization

Eisai GmbHBausch Health Ireland Ltd.

Weill Medical College of Cornell University

+ [5]

Inactive Organization

Ligand Pharmaceuticals, Inc.

Eisai, Inc.

License Organization

Ewopharma AG

Ligand Pharmaceuticals, Inc.

Eisai Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

United States (29 Dec 1999),

Cutaneous T-Cell Lymphoma

RegulationOrphan Drug (Japan)

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Structure/Sequence

Molecular FormulaC24H28O2

InChIKeyNAVMQTYZDKMPEU-UHFFFAOYSA-N

CAS Registry153559-49-0

主要目的：在皮肤T细胞淋巴瘤(CTCL)中国人群中评价贝沙罗汀胶囊单药治疗既往接受至少一次全身治疗的复发或难治性皮肤T细胞淋巴瘤患者的有效性和安全性。次要目的：在CTCL中国人群中进行贝沙罗汀胶囊300mg/m2/d的药代动力学研究。

[Translation]

Primary objective: To evaluate the efficacy and safety of bexarotene capsules as a monotherapy in patients with relapsed or refractory cutaneous T-cell lymphoma (CTCL) who have received at least one previous systemic therapy in the Chinese population with cutaneous T-cell lymphoma (CTCL). Secondary objective: To conduct a pharmacokinetic study of bexarotene capsules 300 mg/m2/d in the Chinese population with CTCL.

Start Date18 Feb 2025

Sponsor / Collaborator

Bushu Pharmaceuticals Ltd.

[+3]

NCT05296304

/ RecruitingPhase 1IIT

A Phase Ib Trial Combining Bexarotene With Ultra-Low Dose Total Skin Electron Beam (Tseb) Radiotherapy For The Treatment Of Diffuse Cutaneous T-Cell Lymphomas

The researchers are doing this study to test the safety of combining bexarotene with TSEB radiotherapy in people who have a common form of CTCL called mycosis fungoides (MF).
Bexarotene is a form of vitamin A that activates proteins called retinoid X receptors, which may stop the growth of cancer cells and kill them. TSEB radiotherapy is a type of radiation therapy that treats the entire surface of the skin with very low doses of radiation to kill cancer cells and shrink tumors. This type of radiation does not pass through the outer layers of the skin into the tissues and organs below the skin.
The study researchers think that giving bexarotene treatment at the same time as treatment with TSEB radiotherapy may be more effective against MF than either treatment given alone or in sequence (one after the other).

Start Date16 Mar 2022

Sponsor / Collaborator

Memorial Sloan Kettering Cancer Center

100 Clinical Results associated with Bexarotene

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100 Translational Medicine associated with Bexarotene

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100 Patents (Medical) associated with Bexarotene

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1,452

Literatures (Medical) associated with Bexarotene

01 May 2025·Talanta

Metabolic signatures by LC-HRMS/MS of jabuticaba (Plinia cauliflora) juice, liqueur, and wines reveal the wealthiest sources of bioactive metabolites

Article

Author: Vaz, Boniek G ; Castro, Sandra B R ; Santos, Gabriel F ; Silva, Patricia A ; Lima, Gesiane S ; Lima, Nerilson M ; de Jesus A S Andrade, Teresinha ; Dias, Leandro S ; Alves, Caio Cesar S ; Carli, Alessandra P

This study aimed to determine the total phenolic content, antioxidant and anti-inflammatory activities, and metabolomic profiling of Jabuticaba beverages. The metabolomic profiling showed a greater abundance of flavonoids in liqueur samples, while sweet wine predominantly contained phenolic acids. On the other hand, dry wine was characterized by a higher abundance of terpenes. The total phenolic content (TPC) was determined by the Folin-Ciocalteu method, while antioxidant activity was evaluated using the DPPH radical-scavenging assay. Notably, dry wine was rich in anthocyanins and tannins and demonstrated the highest TPC (2985.08 ± 0.23 mg GAE/L). Furthermore, this sample exhibited superior antioxidant activity (IC₅₀ 0.83 ± 0.005 μg/mL). All beverages' samples displayed excellent antioxidant potential and TPC ranking as: dry wine > liqueur > sweet wine > juice. In terms of anti-inflammatory activity, treatments with 5 % dry wine led to reduce NO production. Molecular networking and chemometric tools, including HCA and PLS-DA, were employed to differentiate the samples and identify key metabolites. Chemometric analysis showed similar molecular composition between liqueur and dry wine samples, with the primary differences observed in their content of phenolic acids and simple phenols.

01 Apr 2025·Biochemistry

Structural and Mechanistic Insights into the Main Protease (Mpro) Dimer Interface Destabilization Inhibitor: Unveiling New Therapeutic Avenues against SARS-CoV-2

Article

Author: Pareek, Akshay ; Singh, Ankur ; Rani, Ruchi ; Sharma, Gaurav Kumar ; Kumar, Pravindra ; Dhaka, Preeti ; Tomar, Shailly ; Jangid, Kuldeep ; Nehul, Sanketkumar

SARS-CoV-2 variant recurrence has emphasized the imperative prerequisite for effective antivirals. The main protease (Mpro) of SARS-CoV-2 is crucial for viral replication, making it one of the prime and promising antiviral targets. Mpro features several druggable sites, including active sites and allosteric sites near the dimerization interface, that regulate its catalytic activity. This study identified six highly efficacious antiviral SARS-CoV-2 compounds (WIN-62577, KT185, bexarotene, ledipasvir, diacerein, and simepervir) using structure-based virtual screening of compound libraries against Mpro. Using SPR and ITC, the binding of selected inhibitory compounds to the target Mpro was validated. The FRET-based protease assay demonstrated that the identified molecules effectively inhibit Mpro with IC₅₀ values in the range from 0.64 to 11.98 μM. Additionally, in vitro cell-based antiviral assays showed high efficacy with EC₅₀ values in the range of 1.51 to 18.92 μM. The crystal structure of the Mpro-minocycline complex detailed the possible inhibition mechanism of minocycline, an FDA-approved antibiotic. Minocycline binds to an allosteric site, revealing residues critical for the loss of protease activity due to destabilization of molecular interactions at the dimeric interface, which are crucial for the proteolytic activity of Mpro. The study suggests that the binding of minocycline to the allosteric site may play a role in Mpro dimer destabilization and direct the rational design of minocycline derivatives as antiviral drugs.

01 Apr 2025·The Journal of Dermatology

Clinical characterization of mycosis fungoides with abnormal light reactions induced by narrow‐band UVB therapy: A review of a single‐center experience

Article

Author: Furukawa, Fumina ; Shimizu, Tadamichi ; Makino, Teruhiko ; Mizawa, Megumi

AbstractNarrow‐band UVB (NB‐UVB) therapy at a wavelength of 311 nm is often used to treat mycosis fungoides (MF). However, we occasionally encounter cases of erythema induced by low doses of NB‐UVB, known as an abnormal light reaction (ALR). We investigated the incidence of ALR in patients with MF and the association between ALR and clinical and laboratory findings. Forty patients (30 men and 10 women) with MF (excluding patients treated with bexarotene or etretinate) who received NB‐UVB therapy at the Department of Dermatology, University of Toyama, from January to December 2022 were analyzed. ALR was defined as erythema caused by NB‐UVB irradiation of the nonlesional skin at a dose of ≤0.5 J/cm2. ALR occurred in six of 40 patients (15%). The main symptoms of ALR are erythema, irritation, and itching. ALR was observed in patients with Fitzpatrick skin types II and III, and was more common in patients with T2 and T4 disease than in others. The mechanism underlying its occurrence is unknown; however, it has been suggested that ALR is more likely to occur in patients with extensive skin lesions. In addition, treatment can be continued by reducing the dose of NB‐UVB or switching to a 308‐nm excimer laser, even when ALR occurs. Accumulation of additional cases is required because there were only six patients with ALR in this study.

3

News (Medical) associated with Bexarotene

31 Jul 2024

·www.fiercehealthcare.com

Wells Fargo relationship with Express Scripts under scrutiny in new lawsuit

Wells Fargo joins Johnson & Johnson as the most recent company sued over employee prescription drug price management. Wells Fargo is the most recent corporation to get sued, as alleged by former employees, for inadequately overseeing the price workers were forced to pay for prescription drug prices.In a class action lawsuit filed in federal court named Navarro et al v. Wells Fargo Company, employees say the company did not fulfill its fiduciary obligations. Under the Employee Retirement Income Security Act of 1974, employers are required to adequately manage employee benefits programs.The plaintiffs argue Wells Fargo’s management of the prescription drugs program resulted in higher premiums, out-of-pocket costs and limited wage growth because of the prices it agreed to pay Express Scripts, one of its pharmacy benefit managers, for generic drugs.Employees, they say in the suit, were forced to pay nearly $10,000 for a a prescription of fingolimod, used to treat multiple sclerosis, when the generic version could be purchased without insurance for less than a $1,000 at pharmacies like Cost Plus Drugs and Rite Aid. “No prudent fiduciary would agree to make its plan and participants/beneficiaries pay a price that is fifteen times higher than the price available to anyone who just walks into a pharmacy and pays without using their insurance,” the plaintiffs said in the lawsuit.Across approximately 300 generic drugs, Wells Fargo and Express Scripts made employees pay a markup on average of 114.97% what it costs pharmacies to obtain the drugs, the lawsuit alleges. For specialty drugs, employees said they paid a markup of 383% on average.Other prescriptions were far more expensive for employees at Express Scripts’ pharmacy Accredo. Bexarotene gel, available at Rite Aid for $3,750, cost employees nearly $70,000 from Accredo.“The price discrepancies noted herein are illustrative of a pervasive and systematic problem of unreasonable prescription drug charges, despite well-known alternatives available to defendants,” the lawsuit said. Plaintiffs in the lawsuit say Wells Fargo should have received better rates from Express Scripts or a different PBM, guided employees to more cost-effective options or utilized a pass-through PBM that doesn’t use spread pricing.Wells Fargo was also tagged with accusations that it should have operated with more expertise given its standing in the industry. Plaintiffs noted Wells Fargo publishes research on the economics of the pharma industry, hosts an annual healthcare conference with speakers from major PBMs, operates an employee benefits consulting practice and has publicly warned about rising prescription drug costs and business practices by Express Scripts.A similar lawsuit was filed against Johnson & Johnson in February by the same law firm, Fairmark Partners.“This case alleges that Wells Fargo has failed its employees once again, this time by agreeing to obviously unreasonable terms and prices with its PBM that cause workers to vastly overpay for prescription drugs,” said Michael Lieberman, an attorney with Fairmark Partners. “After years of scrutiny and with clear alternatives available, there are no excuses left for a large corporation like Wells Fargo to ignore its legal obligation to identify reasonable prescription drug coverage options for its employees.” Mark Cuban, founder of Cost Plus Drugs, said in a X post that this type of lawsuit can be expected to occur more often.“This lawsuit is going to happen over and over and over with self insured companies until they realize they have to drop their big 3 PBM and use a Pass Through PBM,” he said. “The good news is if they switch they will save money and get control of their claims data.”As well as the Wells Fargo health plan, top human resource employees were also named as defendants in the lawsuit.Wells Fargo and Express Scripts did not immediately respond to a request for comment from Fierce Healthcare.Aon, the broker for Wells Fargo, was also listed in the lawsuit. Express Scripts was not listed as a defendant.

Patent Infringement

26 Oct 2023

·www.prnewswire.com

SciTech Development Announces The Formation of a Distinguished Medical Advisory Board With Top Oncology Specialists

GROSSE POINTE FARMS, Mich., Oct. 26, 2023 /PRNewswire/ -- SciTech Development, LLC, today announced the formation of a distinguished and independent medical advisory board (MAB) comprised of key opinion leaders and world-renowned experts in T-Cell Lymphomas and hematological malignancies. The board will provide strategic and clinical advice for SciTech's outreach and education initiatives within the oncology community. Continue Reading SciTech Medical Advisory Board "SciTech is excited and incredibly proud that this world-class group of medical experts will assist us with innovative insights that enable us to bring ST-001 to patients who have limited options in their cancer treatments," said President and Managing Partner Earle Holsapple. "The clarity they bring in understanding the clinical needs of patients will serve to guide us through the commencement of our phase 1 clinical trial and through our subsequent expedited clinical program." The three medical advisors appointed to the board are Madeleine Duvic, M.D., Larisa Geskin, M.D., and Ajay Gopal, M.D. Madeleine Duvic, MD – "The development of ST-100 is exciting because this new drug holds the promise of improved bioavailability, leading to increased efficacy with low toxicity." Dr. Duvic is a Professor of Medicine and Dermatology practices in Houston, Texas, and holds the Blanche Bender Endowed Chair of Research. Her clinical research includes translational/molecular studies leading to improved therapies for cutaneous T-cell lymphomas. She has written over 500 peer-reviewed papers and a book on Retinoids. She participated in the development of topical and oral tazarotene and bexarotene which both received FDA approval. Larisa J. Geskin, MD, FAAD - "I am thrilled to support SciTech's innovative approach to cancer therapeutics. SciTech's patented nanoparticle platform, SDP, enhances the effectiveness and safety of fenretinide, which has shown promise in treating patients with incurable cutaneous lymphomas in preliminary studies. SciTech's flagship product, ST-001, stands out for its ability to deliver therapeutic doses without toxic side effects, greatly benefiting our patients." Dr. Geskin is a Professor of Dermatology (in Medicine, Division of Hematology-Oncology) at Columbia University Medical Center and the Director of the Comprehensive Cutaneous Oncology Center at the Columbia University Department of Dermatology. Dr. Geskin serves as the Immediate Past-President of the International Society for Cutaneous Lymphomas (ISCL), the Secretary-Treasurer of the US Cutaneous Lymphomas Consortium (USCLC), and the Founding Chair of the New York Cutaneous Lymphoma Consortium (NYCLC), among her many other responsibilities. Ajay K. Gopal, MD - "Based on the encouraging preclinical data from a variety of laboratories, our observed tolerability of fenretinide, and the unmet need in a spectrum of malignancies novel formulations such as ST-001 nanoFenretinide are certainly worthy of further investigation." Dr. Gopal received his undergraduate degree from Duke University and his MD from Emory University. He completed his internal medicine training at Duke University School of Medicine and his oncology training at the University of Washington and Fred Hutchinson Cancer Center, where he currently holds an endowed chair and serves as a Professor and Clinical Research Director for Hematologic Malignancies. Dr. Gopal has over 2 decades of experience in the development of novel therapies for lymphoma, as reflected by over 200 publications in the field, including the first translational and clinical trial data evaluating fenretinide in lymphoma. Contact: Earle Holsapple Email: [email protected] About SciTech Development SciTech Development, LLC is a clinical-stage pharmaceutical company that has developed a patented nanoparticle drug delivery platform (SDP) that maximizes the bioavailability of water-insoluble therapeutics. SciTech's lead drug candidate, ST-001 nanoFenretinide, combines SDP and the drug fenretinide as a new drug product with potentially broad effectiveness in many cancers. For more information about the Company, please visit: SOURCE SciTech Development

Phase 1Executive Change

17 Nov 2022

·medcitynews.com

Two Pharmacy Owners Plead Guilty in $18M Foreign Medicare Fraud Scheme

Two New York pharmacy owners who “exploited the Covid-19 emergency for their own financial gain,” pleaded guilty to an international scheme to submit fraudulent claims to Medicare for cancer medication, the Department of Justice announced Wednesday. Arkadiy Khaimov, 39, of Forest Hills, and Peter Khaim, 42, also of Forest Hills, engaged in an elaborate healthcare scheme involving more than a dozen pharmacies in New York, according to the justice department. The two would submit millions of dollars in fraudulent Medicare claims for expensive cancer drugs that were not prescribed or distributed to patients. The drugs, Targretin gel, made by Bausch and Panretin gel, made by Concordia, were allegedly dispensed during periods when certain pharmacies were closed due to the pandemic. “Khaim, Khaimov, and their co-conspirators exploited the Covid-19 emergency for their own financial gain by using COVID-19-related ‘emergency override’ billing codes to submit additional fraudulent claims for Targretin Gel 1%,” the justice department said in a news release. The scheme started in New York but became a complex international endeavor as the two men attempted to launder money, amounting to more than $18 million. Khaim and Khaimov established shell companies and sham pharmacy wholesale companies to create the illusion they were operating actual businesses. In reality, they were sending funds from the false Medicare claims to the sham companies. Then, the funds were sent to companies in China and distributed to individuals in Uzbekistan. At that point, the two men received some of the funds in cash, the announcement said. They also allegedly sent money from the fraudulent claims to their relatives through cashier’s checks and used the money themselves to purchase property. Both men face a 20-year prison sentence and their separate hearings are scheduled for May 2023. A spokeperson for the Center for Medicare and Medicaid Services did not immediately respond to a request for comment.

Patent Infringement

100 Deals associated with Bexarotene

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External Link

KEGG	Wiki	ATC	Drug Bank
D03106	Bexarotene	L01XX25	DB00307

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Cutaneous T-Cell Lymphoma	United States	Valeant Pharmaceuticals Luxembourg SARL	29 Dec 1999

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
metastatic non-small cell lung cancer	Discovery	Austria	Eisai, Inc.	01 May 2002
metastatic non-small cell lung cancer	Discovery	Spain	Eisai, Inc.	01 May 2002
metastatic non-small cell lung cancer	Discovery	Germany	Eisai, Inc.	01 May 2002
metastatic non-small cell lung cancer	Discovery	France	Eisai, Inc.	01 May 2002
metastatic non-small cell lung cancer	Discovery	United States	Eisai, Inc.	01 May 2002
metastatic non-small cell lung cancer	Discovery	Canada	Eisai, Inc.	01 May 2002
Non-Small Cell Lung Cancer	Discovery	Austria	Eisai, Inc.	01 May 2002
Non-Small Cell Lung Cancer	Discovery	Germany	Eisai, Inc.	01 May 2002
Non-Small Cell Lung Cancer	Discovery	Canada	Eisai, Inc.	01 May 2002
Non-Small Cell Lung Cancer	Discovery	France	Eisai, Inc.	01 May 2002

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


FRI511 (ENDO2023)	Not Applicable	Hypothyroidism	-	Bexarotene	kjvzawgrkn(wpuyrkpqeb) = pauooewzda zyeweerzxm (mjyavlxtny, 0.8 - 1.7) View more	-	05 Oct 2023
P-200 (EORTC_CLTG2023)	Not Applicable	Mycosis Fungoides Add-on	13	Chlormethine gel + Phototherapy	qqfjilewqa(mneedmdsvg) = An ORR in skin increased overtime and was reported in 84.6% at time of best response: 2 patients presented CR and 9 patients PR. Rash is easy managaeble and it did not affect the response to treatment. uguekqispt (boyebtowfo )	Positive	21 Sep 2023
				Chlormethine gel + Mogamulizumab
NCT03323658 (CTgov)	Phase 1	Breast Ductal Carcinoma \| Breast Carcinoma in Situ \| Atypical Lobular Breast Hyperplasia \| Noninfiltrating Intraductal Carcinoma \| Invasive Mammary Carcinoma	24	Bexarotene (Dose Level 1)	zlzwtxpmny(xmuleysfjj) = eemxcbziee eylkpcggog (juyxieejyq, rajbodpmyg - lyqknhucte) View more	-	06 Dec 2022
				Bexarotene (Dose Level 2)	zlzwtxpmny(xmuleysfjj) = esomewniei eylkpcggog (juyxieejyq, scjulrjcij - zukxxkdjpp) View more
ISRCTN14265371 (CCMR One, ECTRIMS2021)	Phase 2	-	31	Bexarotene	ymuajhgbfc(wwiqaihrsm) = significant adverse events were observed on the trial xqkqlktamr (nurhvmesev )	Positive	12 Oct 2021
ISRCTN14265371 (CCMR One, ECTRIMS2021)	Phase 2	Multiple Sclerosis, Relapsing-Remitting	52	Bexarotene	(asygahjycg) = oukvnilyyc jcvoezvhmn (dxwygtgqtm ) View more	-	12 Oct 2021
				Placebo	(asygahjycg) = pntmvhissl jcvoezvhmn (dxwygtgqtm ) View more
CCMR-One (ECTRIMS2020)	Phase 2	Multiple Sclerosis, Relapsing-Remitting	52	Bexarotene 300mg/m2	svmkhrfrfe(tvijwhzemi) = 100% of bexarotene patients experienced central hypothyroidism abvqbhzkgl (rstgobzdrz ) View more	Positive	07 Dec 2020
				Placebo
NCT00615784 (UPCC04407, CTgov)	Phase 2	Acute Myeloid Leukemia	24	Bexarotene	kcaafbekrb(wrapmusumc) = bqoasxpbtd uhaolvvuud (erzvootcrg, rsrpcovgax - kedbqomjpp) View more	-	17 Nov 2020
NCT01007448 (CTgov)	Phase 4	CD30-Positive recurrent or refractory Cutaneous T-Cell Lymphoma	59	Bexarotene	(mfvgdrqifx) = bmdkkdnaag juxirkfhnz (ucygwtbwil, inccvrfevs - weduuxxajo) View more	-	12 Nov 2019
NCT00153842 (CTgov)	Phase 1/2	Advanced Lung Non-Small Cell Carcinoma \| Advanced Lung Adenocarcinoma	33	Carboplatin+Bexarotene+Paclitaxel (Phase IB: Bexarotene 300mg, Paclitaxel and Carboplatin)	ipsrlxabqu(pwmgwotnzb) = vvxunuosmb mfwdpqswzq (lyfrgdqxyj, sczpumovgw - jdcvkviivs)	-	06 Mar 2019
				Carboplatin+Bexarotene+Paclitaxel (Phase IB: Bexarotene 400mg, Paclitaxel and Carboplatin)	ipsrlxabqu(pwmgwotnzb) = gwrdcdwgbw mfwdpqswzq (lyfrgdqxyj, rdcfiyrhsk - qucmxymkdo)