Delving into the Latest Updates on Quetmolimab with Synapse

Overview

Basic Info

Drug Type

Monoclonal antibody

Synonyms

Quetmolimab (USAN)

+ [2]

Target

CX3CL1

Action

antagonists

Mechanism

CX3CL1 antagonists(C-X3-C motif chemokine ligand 1 antagonists)

Therapeutic Areas

Digestive System Disorders

Active Indication

Crohn Disease

Inactive Indication

Primary Biliary CholangitisRheumatoid Arthritis

Originator Organization

Eisai Co., Ltd.

Active Organization

EA Pharma Co., Ltd.

Inactive Organization

Eisai Co., Ltd.

Eisai, Inc.

License Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Sequence Code 263360826L

Source: *****

Sequence Code 263360825H

Source: *****

Author: Namisaki, Tadashi ; Yoshiji, Hitoshi ; Abe, Masanori ; Ohira, Hiromasa ; Kawano, Tetsu ; Ido, Akio ; Harada, Kenichi ; Higashine, Yukari ; Tanaka, Atsushi ; Tsubouchi, Hirohito ; Kamiya, Yuki ; Shimoda, Shinji ; Kakuda, Yuko ; Nakanuma, Yasuni ; Imai, Toshio ; Zeniya, Mikio ; Hojo, Seiichiro ; Umeda, Atsushi

BackgroundWhile ursodeoxycholic acid (UDCA) remains the first-line therapy for primary biliary cholangitis (PBC), the autoimmune nature of PBC underscores the need for treatments targeting immunological pathways that may achieve a cure. E6011, a novel humanized anti-fractalkine monoclonal antibody, has emerged as a potential therapeutic option for PBC. We conducted a randomized, placebo-controlled, double-blind study to evaluate the efficacy and safety of E6011 in patients with PBC with an incomplete response to UDCA.MethodsThe study was composed of 12-week Double-Blind Phase (placebo, E6011 10 mg/kg/month, 15 mg/kg/month, or 10 mg/kg/every other week [eow]) followed by a 52-week Open-Label Phase. The primary endpoint was the percent change in alkaline phosphatase (ALP) at Week 12.ResultsA total of 29 patients were enrolled. Histological evaluation at screening revealed that 83 % of the enrolled patients were classified as Stage 4 according to the Nakanuma Classification. The mean percent changes in ALP at Week 12 were +0.45 % in the placebo, +0.65 % in the 10 mg/kg/month, +1.23 % in the 15 mg/kg/month and +1.19 % in the 10 mg/kg/eow, with no observed trends toward ALP reduction in the E6011 treatment. Based on the interim analysis, the study was discontinued due to a lack of the efficacy. E6011 was generally safe and well tolerated.ConclusionThis study of E6011 failed to meet the primary endpoint in patients with PBC with an incomplete response to UDCA. The advanced histological severity present in more than 80 % of patients at baseline may have contributed to these findings.

01 Mar 2025·Journal of Pharmaceutical and Biomedical Analysis

A simple LC-MS/MS assay for the quantification of E6011, a novel anti-fractalkine monoclonal antibody, in cynomolgus monkey serum - comparison with ligand binding assay

Article

Author: Ono, Haruna ; Kita, Kenji ; Mano, Yuji ; Kojima, Tomoko

E6011 is a monoclonal antibody that is currently under development for the treatment of rheumatoid arthritis. While ligand binding assays (LBAs) are typically employed for the determination of therapeutic antibodies, ultra-performance liquid chromatography with tandem mass spectrometry (UPLC-MS/MS) represents an alternative platform. E6011 in monkey serum was treated with ammonium sulfate to obtain pellets for subsequent processing. The pellets were subjected to denaturalization reduction, alkylation, and tryptic digestion. The resulting signature peptide of E6011, TLADGVPSR, was assayed. The pellet digestion assay was validated in accordance with the established bioanalytical guidelines. E6011 in monkey serum was quantifiable from 3 to 729 µg/mL, with a sample volume of 0.02 mL. The selectivity was confirmed in 12 individual monkey sera. The accuracy and precision were within ± 11.2 % and 15.0 %, respectively. The validated UPLC-MS/MS assay was employed in a pharmacokinetic study in monkeys. After the intravenous dose at 1 mg/kg, E6011 reached the maximum of 27.4 μg/mL, then declined with the half-life of 169 h. The serum E6011 concentrations determined by the UPLC-MS/MS were comparable to those obtained by the LBA with electrochemiluminescence detection. These findings suggest that the established simple UPLC-MS/MS assay is reproducible and can serve as an alternative assay platform.

22 Dec 2023·Modern Rheumatology

Long-term safety and efficacy of E6011, an anti-fractalkine monoclonal antibody, in patients with rheumatoid arthritis inadequately responding to methotrexate

Article

Author: Umehara, Hisanori ; Yasuda, Nobuyuki ; Kitahara, Yasumi ; Torii, Kentaro ; Nanki, Toshihiro ; Hojo, Seiichiro ; Kawakubo, Makoto ; Tanaka, Yoshiya ; Kawano, Tetsu ; Yamanaka, Hisashi ; Takeuchi, Tsutomu ; Imai, Toshio ; Tago, Fumitoshi

ABSTRACTObjectivesTo evaluate the long-term safety and efficacy of E6011, a humanized anti-fractalkine monoclonal antibody, in patients with rheumatoid arthritis (RA) with an inadequate response to methotrexate (MTX).MethodsActive RA patients with an inadequate response to MTX were randomly assigned to the E6011 or placebo group and received the study drug subcutaneously every 2 weeks during a 24-week double-blind study period. Subjects who completed evaluations at Week 24 were rolled over into the extension phase and received open-label E6011 (200 or 400 mg) every 2 weeks until Week 102. The safety analysis was conducted up to Week 104, and the efficacy analysis was conducted up to Week 84.ResultsA total of 169 subjects completed the double-blind treatment phase and were rolled over into the extension phase. In total, 167 (98.8%) subjects experienced any adverse events, and the incidence of treatment-related adverse events was 56.2%. The American College of Rheumatology 20 response rates were observed between 40 and 70% during the extension phase.ConclusionsE6011 was safe and well tolerated with no notable safety concerns up to 102 weeks in RA patients with an inadequate response to MTX.

100 Deals associated with Quetmolimab

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External Link

KEGG	Wiki	ATC	Drug Bank
D11498	-	-	-

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Crohn Disease	Phase 2	Poland	EA Pharma Co., Ltd.	25 Apr 2019
Crohn Disease	Phase 2	Japan	EA Pharma Co., Ltd.	25 Apr 2019
Crohn Disease	Phase 2	Hungary	EA Pharma Co., Ltd.	25 Apr 2019
Crohn Disease	Phase 2	Czechia	EA Pharma Co., Ltd.	25 Apr 2019
Crohn Disease	Phase 2	Russia	EA Pharma Co., Ltd.	25 Apr 2019
Primary Biliary Cholangitis	Discovery	Japan	EA Pharma Co., Ltd.	29 May 2017
Rheumatoid Arthritis	Discovery	Japan	Eisai Co., Ltd.	20 Oct 2016

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03733314 (CTgov)	Phase 2	Crohn Disease	25	E6011 (E6011 10 mg/kg)	amglcpnvyw(flxmqpujtc) = nbiywhqzbb xwzsaymirs (ppsfoqqdpd, yiitwhfcrm - yertkpkogc) View more	-	02 Apr 2025
				Placebo+E6011 (Placebo Then E6011 10 mg/kg)	amglcpnvyw(flxmqpujtc) = zrgsvtzwgd xwzsaymirs (ppsfoqqdpd, nrbnqgwbyf - wjcqdtgqub) View more
NCT02039063 (CTgov)	Phase 1/2	Crohn Disease	28	E6011 (Cohort 1: E6011 2 mg/kg)	(woqktakari) = lnoarbayly wafdogljhn (cdcmgbtlsf, ifmddgncrv - xsoobhvnek) View more	-	30 Jan 2023
				E6011 (Cohort 2: E6011 5 mg/kg)	(woqktakari) = zhwmxlizbf wafdogljhn (cdcmgbtlsf, sxvuvarbut - onekkuvkhq) View more
NCT02960490 (CTgov)	Phase 2	Rheumatoid Arthritis	66	placebo+E6011 (Core Treatment Phase: Placebo)	viyvajpyqm(jlmmjxoawg) = degfzhuedq ulmzonqrui (pysgnmxnys, fbdrgeuyge - veacfgbcig) View more	-	23 Aug 2021
				E6011 (Core Treatment Phase: E6011 400 mg)	viyvajpyqm(jlmmjxoawg) = mmnynkstzj ulmzonqrui (pysgnmxnys, rxdzgvpfzj - kmxtrylusi) View more
NCT02039063 (Pubmed \| J Gastroenterol Hepatol) Manual	Phase 1	Crohn Disease	28	E6011	(vbiwoychly) = vhavivtyks zzoaocjugg (bepoerxxur ) View more	Positive	01 Aug 2021
NCT02960490 (Pubmed \| Isr Med Assoc J) Manual	Phase 2	Rheumatoid Arthritis	64	E6011	(noowkhywtj) = yvogrdulry fvjnuqlcvy (rbtrdpdcln ) View more	Negative	01 Jul 2021
				Placebo	(noowkhywtj) = smdpucibme fvjnuqlcvy (rbtrdpdcln ) View more
NCT02196558 (E6011, CTgov)	Phase 1/2	Rheumatoid Arthritis	53	E6011 (E6011: 100 mg)	(jyucugxfaj) = lchnqncuep yamktcpmxq (jdbhrvcxjp, lpxuascxhg - ftisxzzafz) View more	-	13 Aug 2020
				E6011 (E6011: 200 mg)	(jyucugxfaj) = qxcqfjbtbm yamktcpmxq (jdbhrvcxjp, xfjzkxsrck - uiuyvzxmqx) View more
NCT02960438 (phase 2, EULAR2020)	Phase 2	Rheumatoid Arthritis CX3CR1 + \| CD16 - \| CD56 + ... View more	190	E6011	(fyknqlyiog) = gijuutqnmd ydhvrczvld (oldpcsosti )	Positive	03 Jun 2020
				Placebo	(fyknqlyiog) = njmrtvbzju ydhvrczvld (oldpcsosti )
NCT02960438 (EULAR2019)	Phase 2	Rheumatoid Arthritis CD16+ monocytes	190	E6011 100 mg	(srfbwhbyeo) = cehunsarpv khoizrmqvu (wkgmeeouki )	Positive	12 Jun 2019
				E6011 200 mg	(srfbwhbyeo) = lhemvteqvm khoizrmqvu (wkgmeeouki )
NCT02196558 (EULAR2017)	Phase 1/2	Rheumatoid Arthritis	37	E6011 100 mg	(vsjfqcumyb) = The incidence of adverse event (AE), treatment-related AE and serious AE were 56.8%, 29.7% and 5.4%, respectively. AEs occurring in ≥2 subjects were nasopharyngitis, Injection site erythema, headache and oropharyngeal pain, among which there were no severe AEs, serious infections and deaths. No significant differences were observed in the incidence or severity of AEs across the cohorts. mtrhctwbcs (gnvvnigrtw )	-	14 Jun 2017
				E6011 200 mg

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Quetmolimab

Overview

Basic Info

Structure/Sequence

Related

External Link

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Biosimilar

Regulation