Delving into the Latest Updates on BI-44370 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [3]

Target

CGRP receptor

Mechanism

CALCRL antagonists(Calcitonin gene-related peptide type 1 receptor antagonists)

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

Acute migraine

Originator Organization

C.H. Boehringer Sohn AG & Co. KG

Active Organization-

Inactive Organization

Boehringer Ingelheim GmbH

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC35H47N5O6

InChIKeyHTLWMOKBJQKDIJ-WJOKGBTCSA-N

CAS Registry866086-05-7

Safety, Tolerability and Pharmacokinetics of Multiple Rising Oral Doses of BI 44370 TA Tablets (100 mg, 200 mg and 300 mg Three Times Every Two Hours on One Day and q.d. for Another 2 to 3 Days) in Healthy Male and Female Volunteers, a Randomised, Doubleblind, Placebo-controlled Within Dose Groups Phase I Study

Evaluation of safety, tolerability and pharmacokinetics of multiple rising oral doses of BI 44370 TA in healthy male and female volunteers

Start Date01 Jan 2009

Sponsor / Collaborator

Boehringer Ingelheim GmbH

NCT00743015 / CompletedPhase 1

Relative Bioavailability Following Single Oral Administration of 200 mg of BI 44370 During and Between Migraine Attacks in Male and Female Migraine Patients. An Open-label, Fixed-sequence, Two-period Study With Intraindividual Comparison

The general aim is to evaluate the relative oral bioavailability of BI 44370 TA tablets during and between migraine attacks as well as Safety, Tolerability and Pharmacokinetic

Start Date01 Sep 2008

Sponsor / Collaborator

Boehringer Ingelheim GmbH

NCT02215772 / CompletedPhase 1

A Phase I Trial to Investigate the Metabolism and Pharmacokinetics of an Open Label Single Dose of 200 mg [14C]-BI 44370 BS Administered as an Oral Solution in Healthy Male Volunteers

Study to investigate the basic pharmacokinetics of BI 44370 BS, its metabolite CD 10419 BS, and 14C-radioactivity including mass balance, excretion pathways, and metabolism following a single oral administration of 200 mg [14C]BI 44370 BS to healthy male volunteers and to evaluate safety and tolerability following a single oral administration of 200 mg [14C]BI 44370 BS to healthy male volunteers

Start Date01 Sep 2008

Sponsor / Collaborator

Boehringer Ingelheim GmbH

100 Clinical Results associated with BI-44370

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100 Translational Medicine associated with BI-44370

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100 Patents (Medical) associated with BI-44370

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8

Literatures (Medical) associated with BI-44370

01 Sep 2022·European Journal of Clinical Pharmacology

Safety evaluation of oral calcitonin-gene–related peptide receptor antagonists in patients with acute migraine: a systematic review and meta-analysis

Review

Author: Lee, Seoyeon ; Han, Nayoung ; Staatz, Christine E ; Baek, In-Hwan

OBJECTIVECalcitonin gene-related peptide (CGRP) receptor antagonists have been suggested as novel treatments for acute migraine. This study aimed to use meta-analysis to compare the safety and tolerability of five existing oral CGRP receptor antagonists (BI44370TA, MK-3207, rimegepant, telcagepant, and ubrogepant) with that of a placebo or triptans against acute migraine.METHODSFive prominent databases were searched to identify randomized controlled trials on this topic. The primary safety outcomes of interest were any adverse events (AEs) and treatment-related adverse events (TRAEs), and secondary outcomes were individual events, namely diarrhea, dizziness, dry mouth, fatigue, nausea, paresthesia, somnolence, upper abdominal pain, and vomiting.RESULTSFifteen studies met the eligibility criteria and were examined in detail. Although, compared to placebo, oral CGRP receptor antagonists significantly increased the incidence of any AEs (risk ratio [RR] = 1.15; 95% confidence interval [CI] = 1.07-1.23), there was no difference in the incidence of TRAEs (RR = 1.18; 95% CI = 1.00-1.38). Moreover, CGRP receptor antagonists were safer than triptans with respect to primary safety outcomes, such as any AEs (RR = 0.78; 95% CI = 0.63-0.98) and TRAEs (RR = 0.68; 95% CI = 0.58-0.79).CONCLUSIONDespite oral CGRP receptor antagonists posing a significantly higher risk of AEs when compared to placebo, CGRP receptor antagonists have a favorable safety profile compared to triptans. Our findings inform strategies to enhance safety and tolerability in the treatment of acute migraine.

01 Aug 2020·Brain and BehaviorQ4 · PSYCHOLOGY

Gepants for abortive treatment of migraine: A network meta‐analysis

Q4 · PSYCHOLOGY

ArticleOA

Author: Xiao, Jing ; Tan, Tianlin ; Liu, Yao ; Hong, Peiwei

AbstractObjectivesTo evaluate and compare the efficacy and safety of gepants for abortive treatment of migraine by network meta‐analysis.Materials & MethodsPublications, which were randomized controlled trials (RCTs) about gepants for abortive treatment of migraine, were acquired from Pubmed and Cochrane Library. The literatures screening and quality assessment followed the Cochrane handbook. Review manager 5.3 and Addis v1.16.8 were utilized for data analyzing.ResultsTotally, 15 RCTs were included in the network meta‐analysis. The trials enrolled were with high quality. There are 7 treatments were analyzed: BI 44370 TA, MK‐3207, olcegepant, rimegepant, telcagepant, ubrogepant, and placebo. Of these trials, 11,118 patients and 10,917 patients were assigned to one of 7 treatments randomly for efficacy assessment and safety assessment, respectively. In meta‐analysis of direct comparisons, all gepants were superior to placebo in achieving pain freedom 2 hr postdose and only rimegepant and telcagepant were higher than placebo in incidence of any adverse events. In network meta‐analysis, the rank best 3 drugs were olcegepant, BI 44370 TA, and MK‐3207 for efficacy outcomes. And the rank best 3 drugs were BI 44370 TA, placebo, and ubrogepant for safety outcomes.ConclusionGepants were effective for abortive treatment of migraine. The most effective treatment of gepants for migraine might be olcegepant which were administrated transvenously. And all of gepants were safe for migraine treatment with single dose.

02 Sep 2015·Expert Opinion on Drug Metabolism & ToxicologyQ2 · MEDICINE

Review of dose–response curves for acute antimigraine drugs: triptans, 5-HT_1Fagonists and CGRP antagonists

Q2 · MEDICINE

Review

Author: Tfelt-Hansen, Peer ; Hougaard, Anders

INTRODUCTIONDose-response curves for efficacy and tolerability are the important determinants for the choice of doses of acute migraine drugs.AREAS COVEREDDose-response curves for the efficacy of seven triptans (5-HT1B/1D receptor agonists), a 5-HT1F receptor agonist (lasmiditan) and four oral calcitonin-gene related peptide receptor antagonists (telcagepant, MK-3207, BI 44370 TA and BMS-927711) in placebo-controlled trials were reviewed. In addition, dose-response curves for adverse events (AEs) were reviewed.EXPERT OPINIONFor most triptans, the dose-response curve for efficacy is flat, whereas AEs often increase with increasing doses. The two other groups of drugs also have flat dose-response curves for efficacy. Overall, the triptans still have the most favorable efficacy-tolerability profile. Current acute antimigraine drugs do not fulfill the expectations of the patients, and thus, there are many unmet needs. Although upcoming drugs may not be superior to triptans, migraine patients will potentially benefit greatly from these, especially patients who are triptan non-responders and patients with cardiovascular disease.

100 Deals associated with BI-44370

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB16037

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute migraine	Phase 2	FR	Boehringer Ingelheim GmbH	01 Aug 2008
Acute migraine	Phase 2	GB	Boehringer Ingelheim GmbH	01 Aug 2008
Acute migraine	Phase 2	SE	Boehringer Ingelheim GmbH	01 Aug 2008
Acute migraine	Phase 2	DE	Boehringer Ingelheim GmbH	01 Aug 2008
Acute migraine	Phase 2	SV	Boehringer Ingelheim GmbH	01 Aug 2008
Acute migraine	Phase 2	NL	Boehringer Ingelheim GmbH	01 Aug 2008
Acute migraine	Phase 2	IT	Boehringer Ingelheim GmbH	01 Aug 2008
Acute migraine	Phase 2	ES	Boehringer Ingelheim GmbH	01 Aug 2008
Acute migraine	Phase 2	BE	Boehringer Ingelheim GmbH	01 Aug 2008