Delving into the Latest Updates on TAK-906 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Trazpiroben, ATC-1906, TAK-906 Maleate

Target

D2 receptor x D3 receptor

Action

antagonists

Mechanism

D2 receptor antagonists(Dopamine D2 receptor antagonists), D3 receptor antagonists(Dopamine D3 receptor antagonists)

Therapeutic Areas

Nervous System DiseasesDigestive System DisordersEndocrinology and Metabolic Disease+ [1]

Active Indication-

Inactive Indication

Diabetic GastroparesisGastroparesis

Originator Organization

Takeda Pharmaceutical Co., Ltd.

Active Organization-

Inactive Organization

Millennium Pharmaceuticals, Inc.

Takeda Pharmaceutical Co., Ltd.

License Organization

Takeda Pharmaceutical Co., Ltd.Altos Therapeutics LLC

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC31H39N3O4

InChIKeyBDXJYAAYLZTLEK-UHFFFAOYSA-N

CAS Registry1352993-39-5

The aim of this study is to understand how TAK-906 tablets and capsules are processed by the body in healthy adults under fasting conditions and also how TAK-906 tablets are processed by the body when taken with a high fat high calorie breakfast compared to fasting.
This study will require participants to stay at the clinical research unit for about 3 weeks to be monitored after receiving TAK-906.

Start Date02 Apr 2021

Sponsor / Collaborator

Takeda Pharmaceutical Co., Ltd.

NCT04454918

/ CompletedPhase 1

A Phase 1 Study to Assess Absolute Bioavailability of TAK-906 and to Characterize Mass Balance, Pharmacokinetics, Metabolism, and Excretion of [14C]-TAK-906 in Healthy Male Subjects

The purpose of this study is to determine ABA of TAK-906 following single oral (capsule) administration of 50 milligram (mg) of TAK-906 and single intravenous (IV) microtracer dose administration of 100 microgram (μg) (approximately 1 microcurie [μCi]) of [14C]-TAK-906 in Period 1 (ABA), and to determine the mass balance of TAK-906 in urine and feces following a single oral (solution) administration of 50 mg (approximately 100 μCi) of [14C]-TAK-906 in Period 2 (absorption, distribution, metabolism, and elimination [ADME]).

Start Date30 Jul 2020

Sponsor / Collaborator

Millennium Pharmaceuticals, Inc.

NCT04121078

/ CompletedPhase 1

A Phase 1, Open-Label, Randomized, Two-Way Crossover Study to Evaluate the Effect of Single-Dose Intravenous Rifampin as a Prototypic Inhibitor of OATP1B1 and OATP1B3 on the Single-Dose Pharmacokinetics of Oral TAK-906 in Healthy Adult Subjects

The purpose of this study is to evaluate the effect of single dose intravenous rifampin on the single-dose PK of orally administered TAK-906.

Start Date15 Oct 2019

Sponsor / Collaborator

Millennium Pharmaceuticals, Inc.

100 Clinical Results associated with TAK-906

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100 Translational Medicine associated with TAK-906

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100 Patents (Medical) associated with TAK-906

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10

Literatures (Medical) associated with TAK-906

01 Oct 2023·Neurogastroenterology and motility

Randomized clinical trial: A phase 2b controlled study of the efficacy and safety of trazpiroben (TAK‐906) for idiopathic or diabetic gastroparesis

Article

Author: Huh, Susanna Y. ; Chen, Yaozhu J. ; Tack, Jan ; Zhang, Yanwei ; Mehrotra, Shailly ; Kuo, Braden ; McCallum, Richard ; Parkman, Henry P.

Abstract:

Background:

Previous clinical studies of trazpiroben, a dopamine D2/D3 receptor antagonist for long‐term treatment of moderate‐to‐severe idiopathic and diabetic gastroparesis, have shown improved symptoms of fullness. This study assessed trazpiroben efficacy, safety, and tolerability in adults with idiopathic and diabetic gastroparesis versus placebo.

Methods:

This global, multicenter, double‐blind, parallel‐group, phase 2b study (NCT03544229) enrolled eligible adults aged 18–85 years with symptomatic idiopathic or diabetic gastroparesis. Randomized participants received either oral placebo or trazpiroben 5, 25, or 50 mg, administered twice daily over 12 weeks, and completed the American Neurogastroenterology and Motility Society Gastroparesis Cardinal Symptom Index‐Daily Diary. Change in weekly composite score from baseline to week 12 (primary endpoint) and treatment‐emergent adverse events were assessed. Data were summarized descriptively.

Key Results:

Overall, 242 participants were enrolled (mean [standard deviation] age 55.7 [14.2] years; 75.6% female); 193 completed the study. No significant differences in change from baseline in weekly average of the daily diary composite score occurred at week 12 between placebo (least‐squares mean [standard error] −1.19 [0.12]) and trazpiroben (5, 25, and 50 mg: −1.11 [0.22], −1.17 [0.12], and −1.21 [0.12], respectively). Overall, 41.4% of participants receiving trazpiroben reported treatment‐emergent adverse events (placebo, 39.7%). No serious events were considered trazpiroben‐related; no life‐threatening or fatal events were reported.

Conclusions & Inferences:

There was no clinically meaningful difference in efficacy between trazpiroben and placebo in treating gastroparesis, based on the primary endpoint analysis. Trazpiroben was well tolerated with no new safety concerns identified, strengthening evidence supporting its favorable safety profile.NCT number: NCT03544229.

01 Jun 2022·Clinical pharmacology in drug development

Evaluating the Safety, Tolerability, and Disposition of Trazpiroben, a D₂/D₃ Receptor Antagonist: Phase I Single‐ and Multiple‐Ascending Dose Studies in Healthy Japanese Participants

Article

Author: Hisakuni Sekino ; Kentarou Kudou ; Chunlin Chen ; Takayoshi Yamaguchi ; Hiroyuki Okamoto ; Roger Whiting

Abstract:

Trazpiroben (TAK‐906) is a peripherally selective dopamine D2/D3 receptor antagonist being developed to treat chronic gastroparesis. This phase I, randomized, double‐blind, placebo‐controlled, single‐ and multiple‐ascending dose, parallel‐group study evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of trazpiroben in healthy Japanese men. Findings were compared with those from a prior US trial in healthy individuals. Overall, 24 participants were enrolled into 3 cohorts (each n = 8). Per cohort, 6 participants received trazpiroben (cohort 1, 50 mg; 2, 100 mg; 3, 10 mg) once on day 1 and twice daily on days 3 through 7, and two received placebo. Trazpiroben was well tolerated, with no clinically meaningful adverse events observed. Following single‐ and multiple‐dose administration, trazpiroben was rapidly absorbed and eliminated (mean elimination half‐life, 1.89‐6.45 hours; median time to maximum serum concentration [steady state], 1.00‐1.25 hours). Serum prolactin increased with trazpiroben treatment (mean maximum serum concentration 93.32 ng/mL [10 mg] vs. 10.83 ng/mL [placebo]), illustrating receptor target engagement. Results reflected those from healthy US participants, indicating a lack of differences between these ethnic populations in trazpiroben disposition and safety profile. Trazpiroben may represent a promising therapy for chronic gastroparesis across different populations, with further evaluation ongoing in a phase IIb study (NCT03544229).

01 Jun 2022·CTS-Clinical and Translational ScienceQ3 · MEDICINE

The pharmacokinetics of oral trazpiroben (TAK‐906) after organic anion transporting polypeptide 1B1/1B3 inhibition: A phase I, randomized study

Q3 · MEDICINE

ArticleOA

Author: Wang, Lisi ; Huh, Susanna Y. ; Chen, Chunlin ; Dukes, George ; Almansa, Cristina ; Nishihara, Mitsuhiro ; Tolkoff, Max ; Mukker, Jatinder K. ; Ramsden, Diane

Abstract:

Trazpiroben is a dopamine D2/D3 receptor antagonist under development for the treatment of gastroparesis. This phase I, open‐label, randomized, two‐way crossover study (NCT04121078) evaluated the effect of single‐dose intravenous rifampin, a potent inhibitor of the organic anion transporting polypeptides (OATPs) 1B1 and 1B3, on the pharmacokinetics and safety of trazpiroben in healthy adults. The utility of coproporphyrin (CP) I and CPIII as biomarkers of OATP inhibition was also assessed. Overall, 12 participants were enrolled and randomized (1:1) into one of two treatment sequences (AB and BA). Participants received either a single oral dose of trazpiroben 25 mg (treatment A) or a single oral dose of trazpiroben 25 mg immediately after a single 30‐min intravenous infusion of rifampin 600 mg (treatment B). After a washout period of at least 7 days, participants received the other treatment. Geometric mean area under the curve from time 0 extrapolated to infinity (AUC∞) and maximum serum concentration (Cmax) of plasma trazpiroben were higher in participants receiving treatment B than those receiving treatment A (AUC∞, 168.5 vs. 32.68 ng*h/ml; Cmax, 89.62 vs. 14.37 ng/ml); corresponding geometric mean ratios (90% confidence interval) showed 5.16 (4.25–6.25) and 6.24 (4.62–8.42)‐fold increases in these parameters, respectively. In this study, trazpiroben was confirmed as a substrate of OATP1B1/1B3, and therefore co‐administration of trazpiroben with moderate to strong inhibitors of OATP1B1/1B3 is not recommended. This is also the first assessment of the utility of CPI and CPIII as endogenous biomarkers of OATP1B1/1B3 inhibition after a single intravenous dose of rifampin.

2

News (Medical) associated with TAK-906

13 May 2026

·www.fiercebiotech.com

Takeda 0 for 4 against nausea and vomiting after axing another asset

At the start of 2022, Takeda was developing three peptide agonists in nausea and vomiting.\n Takeda has ended development of its nausea and vomiting drug candidate for strategic reasons, continuing its multi-year struggles in the therapeutic area. The nausea and vomiting prospect, TAK-004, completed a phase 1 trial last year. Takeda ran the study to evaluate the safety and tolerability of the investigational peptide agonist while evaluating its effect on the heart rate and blood pressure of healthy adults. The Japanese drugmaker named assessing whether TAK-004 causes an immune response as another objective of the trial.Takeda removed (PDF) the drug candidate from its pipeline as part of its fourth-quarter results, telling investors that it ended TAK-004 development “due to strategic consideration.” The company’s strategy has veered away from nausea and vomiting in recent years.At the start of 2022, Takeda was developing (PDF) three peptide agonists—TAK-105, TAK-510 and TAK-951—in nausea and vomiting, plus its gastroparesis candidate TAK-906. Takeda stopped (PDF) work on the treatment for gastroparesis, a condition associated with nausea and vomiting, early in 2022 in response to phase 2b data. The drugmaker ended (PDF) development of TAK-510 in late 2022 after concluding that the phase 1 data didn’t support further trials. Takeda reached (PDF) the same conclusion about TAK-105 in 2023. Work on the phase 2 candidate TAK-951 continued into 2024. However, in May 2024, Takeda axed the program after the clinical data failed to support further development. The removal of TAK-951 from the pipeline left Takeda without a program targeting nausea and vomiting for the first time in years. Takeda moved (PDF) TAK-004 into human testing in late 2024, re-entering nausea and vomiting clinical development, but the candidate had the same fate as its predecessors. Takeda continues \"to have interest in nausea and vomiting where we see meaningful unmet need,\" a spokesperson said via email.The drugmaker disclosed the discontinuation of TAK-004 development alongside other pipeline updates. The Japanese pharma removed the 5% formulation of TAK-961, its late-phase autoimmune encephalitis candidate, from the pipeline but still plans to seek approval for the 10% product. Data on the 5% formulation will support approval filings for the 10% product, the company said.Takeda removed the Denali Therapeutics-partnered frontotemporal dementia candidate, TAK-594, from its pipeline after ending its alliance with the biotech. The other updates affected approved products, with Takeda ending a booster program for its dengue vaccine Qdenga in light of durability data and axing a proposed indication for the enzyme replacement therapy Adzynma for strategic reasons.

VaccinePhase 2Phase 1PDC

13 May 2026

·firstwordpharma.com

Takeda expands cost-cutting drive with 4500 roles on the line

Takeda was among the biggest pharma downsizers in the first quarter and had already warned that more cuts were coming.Now, the Japanese drugmaker has detailed a new "transformation programme" expected to affect roughly 4500 roles in fiscal 2026 as it looks to centralise corporate functions, trim management layers and simplify operations.The restructuring, unveiled during Takeda's quarterly earnings presentation on Wednesday, is projected to generate more than JPY 200 billion ($1.3 billion) in annualised savings by fiscal 2028. The company will book roughly JPY 170 billion in restructuring charges along the way, but expects to pocket around JPY 100 billion in savings this year alone.The move follows a steady stream of Takeda layoffs since it undertook an enterprise-wide restructuring programme about two years ago. Earlier this year, it disclosed plans to eliminate 634 positions in the US, including 247 jobs in Massachusetts and another 387 roles spread across other states.The cuts came less than six months after Takeda axed 137 jobs tied to its withdrawal from cell therapy development. Those reductions followed an even larger wave in 2024, when the company cut nearly 1000 positions in Massachusetts alone.'New era'"Based on my leadership team, we've updated the organisational structure to transform the company for accelerated speed and growth," said CEO-elect Julie Kim, who takes the reins from Christophe Weber in June, during the company's earnings call. "This has included reducing layers to bring teams closer to patients and customers, centralising and streamlining corporate functions, and driving greater efficiency through data, technology, and AI."Share added, "In addition to our Takeda executive team, our broader governance structure…provides a strong and stable foundation for this new era."Eye on trio of launchesTakeda said savings from the restructuring will be reinvested to help support a trio of upcoming launches; namely, oveporexton (TAK-861), which could hit the market in the second half as the first orexin agonist approved for narcolepsy type 1 if the FDA signs off on it in the third quarter; rusfertide, a potential first‑in‑class hepcidin mimetic for polycythemia vera that is also awaiting an FDA decision and possible launch next half; and zasocitinib, an oral TYK2 inhibitor for psoriasis that Takeda is planning to file this year for a possible commercial debut in the first half of 2027.Kim said that "the convergence of these catalysts offers a timely opportunity to lay out the path forward for our next chapter of growth," which will come in two stages.The first — referred to as "Horizon One" — has a two- three-year timeframe and centres on establishing oveporexton, rusfertide and zasocitinib as the company's growth drivers. "Horizon Two" will focus on accelerating that growth. This is where the company will be "shifting from our maturing portfolio to a new cohort of blockbuster brands…by scaling our first wave of launches while preparing for and executing the launch of our next wave of late-stage assets," Kim said.Pipeline pruningSome assets won't be going along for the ride, however. Takeda provided an update to its pipeline, including curtailing Phase I development of TAK-004 for nausea and vomiting "due to strategic consideration." The drug's fate mirrors that of a number of the company's nausea and vomiting candidates, such as TAK-105 and TAK-510, as well as TAK-906 in the associated condition of gastroparesis.The drugmaker also disclosed that it will stop Phase III work on the 5% formulation of TAK-961, also known as Glovenin-I, in autoimmune encephalitis. Takeda cited "portfolio/filing strategy" for the decision, noting that data on the formulation will support plans to seek approval of the 10% version of the immunoglobulin.The company also confirmed the removal of TAK-594 from its pipeline for frontotemporal dementia, having ended a co-development partnership with Denali Therapeutics earlier in the year.Looking ahead to the upcoming fiscal year ending March 2027, Takeda said it anticipates full-year revenues of JPY 4.64 trillion and profit of JPY 166 billion.-Matt Dennis contributed to this report.

Phase 1Drug ApprovalPhase 3Phase 2

100 Deals associated with TAK-906

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetic Gastroparesis	Phase 2	United States	Millennium Pharmaceuticals, Inc.	26 Sep 2017
Gastroparesis	Phase 2	United States	Millennium Pharmaceuticals, Inc.	26 Sep 2017

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03544229 (CTgov)	Phase 2	Gastroparesis \| Diabetic Gastroparesis	242	Placebo (Placebo)	altyzpwreq(qlmjorfeki) = kxknzaeeob iafohdkbzw (iqqanaqgqj, 0.120) View more	-	16 Nov 2022
				TAK-906 Maleate (TAK-906 Maleate 5 mg)	altyzpwreq(qlmjorfeki) = hxdrefxgde iafohdkbzw (iqqanaqgqj, 0.219) View more
NCT04121078 (Pubmed \| Clin Transl Sci)	Phase 1	coproporphyrin (CP) I \| CPIII	12	Trazpiroben 25 mg	rjjbywrbjt(oisiwobgem) = gznkfctldu ipsjruotqe (qcmcznwxic ) View more	-	01 Jun 2022
				Trazpiroben 25 mg + Rifampin 600 mg	rjjbywrbjt(oisiwobgem) = rtplwtluci ipsjruotqe (qcmcznwxic ) View more
NCT04454918 (CTgov)	Phase 1	-	6	[14C]-TAK-906+TAK-906 (TAK-906 50 mg + [14C]-TAK-906 100 μg)	nirbchhmzm(jzfkyuwlin) = lqbkvampot xwegmjcktc (okcvbtpnkb, cfhzxzzazf - zwozeamwgq) View more	-	07 Mar 2022
				[14C]-TAK-906 ([14C]-TAK-906 50 mg)	xswrdlaypu(rxymmoquud) = zrbxsotcft kfzvdxzoqr (sbwmdifhat, 21.8) View more
NCT03849690 (Pubmed \| Clin Transl Sci)	Phase 1	-	12	Trazpiroben 25 mg alone	sglfetdyii(vihqononvh) = xvnetwbrzq fudflxtfkg (mrjtumjezl ) View more	Positive	26 Feb 2022
				Trazpiroben 25 mg + Esomeprazole 40 mg	sglfetdyii(vihqononvh) = vzicgeoofl fudflxtfkg (mrjtumjezl ) View more
NCT03544229 (Pubmed)	Phase 1	-	24	Trazpiroben	ohlkanxpqd(awvccmevvr) = Trazpiroben was well tolerated, with no clinically meaningful adverse events observed zudwtslgue (zjccjqejzr )	-	29 Dec 2021
				Placebo
NCT04121078 (CTgov)	Phase 1	-	12	TAK-906 (Treatment A: TAK-906 25 mg)	mnjbwcvvrp(citnrkbcmy) = fwsslsvvhr bjxbyqfijp (sgwcaznjtc, 38.7) View more	-	09 Dec 2020
				Rifampin+TAK-906 (Treatment B: Rifampin 600 mg and TAK-906 25 mg)	mnjbwcvvrp(citnrkbcmy) = hmylwwchyf bjxbyqfijp (sgwcaznjtc, 68.6) View more
NCT03849690 (CTgov)	Phase 1	-	12	TAK-906 (TAK-906 25 mg)	uefvlmdrcg(nvochdusbt) = fdvdkicyjh qicsrmavsn (cemxomqyaz, 36.5) View more	-	12 May 2020
				Esomeprazole+TAK-906 (Esomeprazole 40 mg and TAK-906 25 mg)	uefvlmdrcg(nvochdusbt) = hdyekrpzcu qicsrmavsn (cemxomqyaz, 40.5) View more
NCT03268941 (CTgov)	Phase 2	Gastroparesis \| Diabetic Gastroparesis	51	TAK-906 Maleate Placebo (Part 1: Placebo)	hsqwateiqg = prjqsmqbjg fsqdeaqjjn (mlfqllztbz, awgrqywxgb - yjdvcubryd) View more	-	23 Jul 2019
				TAK-906 Maleate (Part 1: TAK 906 Maleate 5 mg)	hsqwateiqg = jcjcitcgvp fsqdeaqjjn (mlfqllztbz, qjvqmhfagd - wutvsqsqfh) View more
NCT03237156 (CTgov)	Phase 1	-	24	placebo+TAK-906 (Cohorts 1-3: Placebo)	ycxlmcaddv = jtennrluor kfnptyzbkv (ljtaqogqcz, xseufvqjod - sbywvnxdaf) View more	-	18 Feb 2019
				TAK-906 (Cohort 1: TAK-906 50 mg)	ycxlmcaddv = qgsfottuvr kfnptyzbkv (ljtaqogqcz, zdeeijpwdi - preqjosmgg) View more
NCT03161405 (CTgov)	Phase 1	-	12	TAK-906 Maleate (TAK-906 Maleate 25 mg)	gbgkpdahsf(cxwfgzxbid) = xqnlzhrcht wtiujzyjhl (psnlgaffek, 4.6337) View more	-	11 Jan 2019
				Itraconazole+TAK-906 Maleate (Itraconazole 200 mg + TAK-906 Maleate 25 mg)	gbgkpdahsf(cxwfgzxbid) = zcyaiqvgel wtiujzyjhl (psnlgaffek, 4.8780) View more