Atogepant. Calcitonin gene-related peptide (CGRP) receptor antagonist,
                        Preventive treatment of migraine

Martelletti, Paolo; Cipolla, Fabiola; Capi, Matilde; Curto, M; Lionetto, Luana

doi:10.1358/dof.2020.45.5.3123467

Cited by 17 publications

(14 citation statements)

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“…Chemically, it contains six fluorine atoms, and its synthesis [ 76 , 77 ] is shown in Scheme 16 . The synthesis starts from 5-bromo-6-methylpyridin-2-ol ( 119 ), which is N -alkylated with 2,2,2-trifluoroethyl triflate to afford derivative 121 .…”

Section: New Halogen-containing Drugsmentioning

confidence: 99%

“…Catalytic hydrogenation (PtO 2 ) in MeOH of 123 gave the piperidinone 124 , which was firstly lithiated by LiHMDS and, secondly, converted to the corresponding azide by using 2,4,6-triisopropylbenzenesulfonyl azide ( 125 ) to give 126 . The concomitant reduction to amine and BOC protection of intermediate 126 followed by Supercritical fluid chromatography (SFC) yielded the intermediate 127 , which underwent BOC removal ( 128 ) and condensation with carboxylic acid synthon 129 [ 76 ] to afford atogepant ( 130 ). Different routes for the preparation of synthon 129 have been proposed [ 77 ].…”

Section: New Halogen-containing Drugsmentioning

confidence: 99%

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New Halogen-Containing Drugs Approved by FDA in 2021: An Overview on Their Syntheses and Pharmaceutical Use

et al. 2022

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This review describes the recent Food and Drug Administration (FDA)-approved drugs (in the year 2021) containing at least one halogen atom (covalently bound). The structures proposed throughout this work are grouped according to their therapeutical use. Their synthesis is presented as well. The number of halogenated molecules that are reaching the market is regularly preserved, and 14 of the 50 molecules approved by the FDA in the last year contain halogens. This underlines the emergent role of halogens and, in particular, of fluorine and chlorine in the preparation of drugs for the treatment of several diseases such as viral infections, several types of cancer, cardiovascular disease, multiple sclerosis, migraine and inflammatory diseases such as vasculitis.

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Section: New Halogen-containing Drugsmentioning

confidence: 99%

Section: New Halogen-containing Drugsmentioning

confidence: 99%

New Halogen-Containing Drugs Approved by FDA in 2021: An Overview on Their Syntheses and Pharmaceutical Use

et al. 2022

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“…Alanine transaminase or aspartate aminotransferase were found >3× the upper limit normal (ULN) in 1.7% (placebo group), 2.2% (10 mg QD), 0.6% (30 mg QD), 1.7% (60 QD), 1.2% (30 mg BID) and 1.1% (60 mg BID). The results indicate that atogepant is well tolerated and drug-related serious AEs were absent [ 21 ].…”

Section: Preventative New Gepantsmentioning

confidence: 99%

CGRP Receptor Antagonists and 5-HT1F Receptor Agonist in the Treatment of Migraine

Capi¹,

Angelis

Bernardini³

et al. 2021

JCM

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Discovering that calcitonin-related peptide (CGRP) plays a key role in the complex pathophysiology of migraine has allowed us to make great strides in the development of new approaches for acute and preventive treatment. This evidence has led to the development of small molecules antagonist molecules of the CGRP receptor (“gepants”) and of a new class of medications called “Ditans”. This review presents the data from clinical trials reporting the efficacy, safety, and tolerability of the new drugs used in the treatment of migraines. Evidences show that therapeutic approaches targeted to CGRP have the potential to transform the clinical management of migraine, even though its appropriate place has yet to be determined with accuracy.

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“…Interestingly, rimegepant is currently undergoing a clinical trial for approval as a prophylactic treatment (phase II/III trial, NCT0372368) [48]. The seventh CGRP receptor antagonist, atogepant (MK-8031, AGN-241,689) is the first gepant specifically developed for the prophylaxis of episodic and chronic migraine [49][50][51][52].…”

Section: Blockade Of Cgrp or Its Receptor As A Treatment For Migrainementioning

confidence: 99%

“…a CGRP receptor antagonist with a higher potency and longer half-life than ubrogepant (which is used for the acute treatment of migraine). For this reason, its use has been proposed for the prevention of episodic and chronic migraine (see Table 1) [49][50][51][52].…”

Section: Atogepant Atogepant (Mk-8031 or Agn-241689) Ismentioning

confidence: 99%

CGRP inhibitors for migraine prophylaxis: a safety review

Rivera‐Mancilla

Villalón

MaassenVanDenBrink

2020

Expert Opinion on Drug Safety

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Introduction: Since calcitonin gene-related peptide (CGRP) plays an important role in the pathophysiology of migraine via the activation of the trigeminovascular system, the newest prophylactic treatments directly block CGRP or its receptor. However, the safety of these novel antimigraine drugs is not yet sufficiently established. Areas covered: Based on the blockade of CGRP or its receptor, this review considers: (i) the effects of the novel prophylactic antimigraine drugs (i.e. gepants and monoclonal antibodies) in clinical trials; and (ii) the potentially negative effects of blocking CGRP or its receptor in terms of safety. Expert opinion: In the last decade, clinical trials have demonstrated the efficacy of new drugs for the preventive treatment of migraine which aim to (i) block CGRP or its receptor; (ii) increase tolerability as compared to the currently available prophylactics; and/or (iii) be more effective and safer than other treatments. However, these trials are limited to study the safety on the short term, and a cardiovascular risk with prolonged use cannot be excluded. Clearly, basic science experimental studies and long-term clinical trials (i.e. Phase IV) are required to delineate the safety of the newest prophylactic antimigraine drugs without causing unwanted side effects due to chronic CGRP (receptor) blockade.

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Atogepant. Calcitonin gene-related peptide (CGRP) receptor antagonist, Preventive treatment of migraine

Cited by 17 publications

References 0 publications

New Halogen-Containing Drugs Approved by FDA in 2021: An Overview on Their Syntheses and Pharmaceutical Use

New Halogen-Containing Drugs Approved by FDA in 2021: An Overview on Their Syntheses and Pharmaceutical Use

CGRP Receptor Antagonists and 5-HT1F Receptor Agonist in the Treatment of Migraine

CGRP inhibitors for migraine prophylaxis: a safety review

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