Delving into the Latest Updates on BI-764198 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

[4-(6-aminopyridazin-3-yl)piperidin-1-yl][5-(4-fluorophenoxy)-4-methoxypyridin-2-yl]methanone, BI 764198, BI-764198

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Target

TRPC6

Action

antagonists

Mechanism

TRPC6 antagonists(transient receptor potential cation channel subfamily C member 6 antagonists)

Therapeutic Areas

Urogenital DiseasesOther Diseases

Active Indication

Glomerulosclerosis, Focal SegmentalChronic Kidney DiseasesGlomerular disease

Inactive Indication

COVID-19Respiratory DiseasesRespiratory Distress Syndrome, Acute

Originator Organization

Boehringer Ingelheim International GmbH

Active Organization

Boehringer Ingelheim GmbHAlmac Pharma Services Ltd.Boehringer Ingelheim International GmbH

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Inactive Organization-

License Organization-

Drug Highest PhasePhase 3

First Approval Date-

RegulationOrphan Drug (European Union), Breakthrough Therapy (China), Orphan Drug (Japan)

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A Multicentre, Randomised, Double-blind, Parallel Group, Placebo-controlled Trial to Assess the Effects of Oral TRPC6 Inhibitor BI 764198 Taken Over a 104 Week Treatment Period in Adult and Adolescent Participants With Primary Focal Segmental Glomerulosclerosis (pFSGS) or Genetic FSGS Related to TRPC6 Gene Variants

This study is open to adults and adolescents with a kidney condition called focal segmental glomerulosclerosis (FSGS). The purpose of this study is to find out whether a medicine called BI 764198 helps people with FSGS.
Participants are put into 2 groups randomly, which means by chance. Every participant has an equal chance of being in each group. One group takes BI 764198 tablets, and the other group takes placebo tablets. Placebo tablets look like BI 764198 tablets but do not contain any medicine.
Participants take a tablet once a day for up to 2 years. All participants also continue their standard medication for FSGS.
Participants are in the study for up to 2 years. During this time, they visit the study site about every 3 months. Participants regularly collect urine samples. This is done to check their kidneys. The results are compared between the two groups to see whether the treatment works. The doctors also regularly check participants' health and take note of any unwanted effects.

Start Date19 Dec 2025

Sponsor / Collaborator

Boehringer Ingelheim GmbH

NCT06955754

/ CompletedPhase 1

Relative Bioavailability of Three Different Oral Formulations of BI 764198 Including the Investigation of Food Effect on the Tablet Formulation in Healthy Male and Female Subjects (an Open-label, Randomised, Four-way Crossover Trial)

This trial aims to investigate the relative bioavailability of three different oral formulations of BI 764198 and how this is influenced by food.

Start Date20 May 2025

Sponsor / Collaborator

Boehringer Ingelheim GmbH

100 Clinical Results associated with BI-764198

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100 Translational Medicine associated with BI-764198

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100 Patents (Medical) associated with BI-764198

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2

Literatures (Medical) associated with BI-764198

04 May 2025·EXPERT OPINION ON INVESTIGATIONAL DRUGS

A randomized, Phase I study of the safety, tolerability, and pharmacokinetics of BI 764198, a transient receptor potential channel 6 (TRPC6) inhibitor, in healthy Japanese men

Article

Author: Tachibana, Yoshifumi ; Retlich, Silke ; Soleymanlou, Nima ; Sarashina, Akiko ; Yonemura, Takuma

BACKGROUND:

BI 764198 is a selective, oral transient receptor potential cation channel, subfamily C, member 6 inhibitor under investigation for focal segmental glomerulosclerosis.

RESEARCH DESIGN AND METHODS:

Phase I study in 44 Japanese male volunteers. Single dose part: BI 764198 20 mg (n = 6) vs. placebo (n = 2); multiple dose part: BI 764198 40, 80, or 160 mg (n = 9 each) or placebo (n = 9) as a single dose then multiple daily dosing for 2 weeks. Primary endpoint: participants with drug-related adverse events (DRAEs); secondary endpoints: pharmacokinetic.

RESULTS:

DRAEs were reported in 20.5% (9/44) of participants (total BI 764198 21.2% [7/33]; placebo 18.2% [2/11]), mostly diarrhea (total BI 764198 15.2% [5/33]; placebo 18.2% [2/11]) and headache (BI 764198 80 mg 11.1% [1/9]; BI 764198 160 mg 33.3% [3/9]). BI 764198 exposure increased near dose proportionally to 80 mg and was slightly higher than anticipated with 160 mg. Pharmacokinetics were similar in Asians and non-Asians after accounting for body weight. Limitations include small sample size per dose and short trial duration.

CONCLUSIONS:

BI 764198 was well tolerated; exposure increased near dose proportionally to 80 mg, as previously observed in predominantly White volunteers.

CLINICAL TRIAL REGISTRATION:

This study was registered on Clinical Trials.gov, identifier NCT04665700.

01 Aug 2023·Thorax

TRPC6 inhibitor (BI 764198) to reduce risk and severity of ARDS due to COVID-19: a phase II randomised controlled trial

Article

Author: Diaz, George A ; Welte, Tobias ; Estrada, Vicente ; Soleymanlou, Nima ; Lacamera, Peter ; Gupta, Abhya ; McAuley, Danny Francis ; Ware, Lorraine B ; Choi, Wansuk ; Kaste, Renee

Background:

Despite the availability of COVID-19 vaccinations, there remains a need to investigate treatments to reduce the risk or severity of potentially fatal complications of COVID-19, such as acute respiratory distress syndrome (ARDS). This study evaluated the efficacy and safety of the transient receptor potential channel C6 (TRPC6) inhibitor, BI 764198, in reducing the risk and/or severity of ARDS in patients hospitalised for COVID-19 and requiring non-invasive, supplemental oxygen support (oxygen by mask or nasal prongs, oxygen by non-invasive ventilation or high-flow nasal oxygen).

Methods:

Multicentre, double-blind, randomised phase II trial comparing once-daily oral BI 764198 (n=65) with placebo (n=64) for 28 days (+2-month follow-up). Primary endpoint: proportion of patients alive and free of mechanical ventilation at day 29. Secondary endpoints: proportion of patients alive and discharged without oxygen (day 29); occurrence of either in-hospital mortality, intensive care unit admission or mechanical ventilation (day 29); time to first response (clinical improvement/recovery); ventilator-free days (day 29); and mortality (days 15, 29, 60 and 90).

Results:

No difference was observed for the primary endpoint: BI 764198 (83.1%) versus placebo (87.5%) (estimated risk difference –5.39%; 95% CI –16.08 to 5.30; p=0.323). For secondary endpoints, a longer time to first response (rate ratio 0.67; 95% CI 0.46 to 0.99; p=0.045) and longer hospitalisation (+3.41 days; 95% CI 0.49 to 6.34; p=0.023) for BI 764198 versus placebo was observed; no other significant differences were observed. On-treatment adverse events were similar between trial arms and more fatal events were reported for BI 764198 (n=7) versus placebo (n=2). Treatment was stopped early based on an interim observation of a lack of efficacy and an imbalance of fatal events (Data Monitoring Committee recommendation).

Conclusions:

TRPC6 inhibition was not effective in reducing the risk and/or severity of ARDS in patients with COVID-19 requiring non-invasive, supplemental oxygen support.

Trial registration number:

NCT04604184.

100 Deals associated with BI-764198

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Glomerulosclerosis, Focal Segmental	Phase 3	United States	Boehringer Ingelheim GmbH	19 Dec 2025
Glomerulosclerosis, Focal Segmental	Phase 3	China	Boehringer Ingelheim GmbH	19 Dec 2025
Glomerulosclerosis, Focal Segmental	Phase 3	Japan	Boehringer Ingelheim GmbH	19 Dec 2025
Glomerulosclerosis, Focal Segmental	Phase 3	Argentina	Boehringer Ingelheim GmbH	19 Dec 2025
Glomerulosclerosis, Focal Segmental	Phase 3	Australia	Boehringer Ingelheim GmbH	19 Dec 2025
Glomerulosclerosis, Focal Segmental	Phase 3	Belgium	Boehringer Ingelheim GmbH	19 Dec 2025
Glomerulosclerosis, Focal Segmental	Phase 3	Brazil	Boehringer Ingelheim GmbH	19 Dec 2025
Glomerulosclerosis, Focal Segmental	Phase 3	Croatia	Boehringer Ingelheim GmbH	19 Dec 2025
Glomerulosclerosis, Focal Segmental	Phase 3	Denmark	Boehringer Ingelheim GmbH	19 Dec 2025
Glomerulosclerosis, Focal Segmental	Phase 3	France	Boehringer Ingelheim GmbH	19 Dec 2025

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05213624 (ASN2025)	Phase 2	Glomerulosclerosis, Focal Segmental	60	BI 764198	kzuwrfgiku(tzdgthakfh) = uljtswelhp wzrbsuubob (wlxdtfhsef )	Positive	08 Nov 2025
				BI 764198	kzuwrfgiku(tzdgthakfh) = sxcwfkeovu wzrbsuubob (wlxdtfhsef )
NCT04102462 \| NCT03854552 \| NCT04176536 \| NCT04656288 (Phase 1 trials of BI 764198, Pubmed \| Expert Opin Investig Drugs)	Phase 1	Renal Insufficiency	54	BI 764198	ohlerblsgn(ulzifsuiwa) = 1 participant (16.7%) experienced diarrhea toqtptvprk (szrwojpdhp ) View more	Positive	08 Jun 2025
				Placebo
NCT04665700 (Pubmed \| Expert Opin Investig Drugs)	Phase 1	TRPC6	44	BI 764,198 20 mg	pmqcehqomw(aydjkixjhk) = urggnsgffw nvnipssykd (kpqsdhsoiv ) View more	-	04 May 2025
				Placebo	pmqcehqomw(aydjkixjhk) = umhcwaiyjx nvnipssykd (kpqsdhsoiv ) View more
NCT04604184 (Pubmed)	Phase 2	COVID-19	-	BI 764198	egmpibdpbh(ueqalwwxjn): days = 3.41 (95% CI, 0.49 - 6.34) View more	Negative	06 Apr 2023
				Placebo
NCT04604184 (CTgov)	Phase 2	COVID-19 \| Respiratory Distress Syndrome, Acute	133	BI 764198 (BI 764198 Treatment Group)	anqcdgwsze = gvorwccuib zblsjktxyn (awrurdbdqo, ptllomtfcm - ifwlaakzxp) View more	-	11 Apr 2022
				Placebo (Placebo)	anqcdgwsze = yqbnmevrcg zblsjktxyn (awrurdbdqo, vbdrxxzsma - lowblytsuf) View more