BCX-4161, a Small Molecule and Orally Bioavailable Plasma Kallikrein Inhibitor for the Treatment of Hereditary Angioedema

Bantia, Shanta; Zhang, Jianwen; Wilson, Ramanda; Parker, Cynthia; Kellogg, Debra; Kotian, Pravin L.; Babu, Y.S.

doi:10.1016/j.jaci.2012.12.1425

Cited by 7 publications

(6 citation statements)

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“…Other manufacturers of C1‐INH are also evaluating formulations for subcutaneous long‐term prophylaxis. Biocryst is working on oral kallikrein inhibitors, which inhibit plasma kallikrein and suppress bradykinin production . First results from clinical trials are promising .…”

Section: Discussionmentioning

confidence: 99%

Prophylaxis in hereditary angioedema (HAE) with C1 inhibitor deficiency

Greve

Straßen

Gorczyza

et al. 2016

J Deutsche Derma Gesell

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SummaryHereditary angioedema (HAE) is a rare congenital disorder characterized by recurrent episodes of subcutaneous or submucosal edema. Laryngeal manifestations can be life-threatening. In the majority of cases, the disease can be adequately treated with an on-demand approach -in some cases, however, short-or long-term prophylaxis is indicated. Attenuated androgens used to be the drugs of choice, but they are associated with considerable side effects and no longer commercially available in the German-speaking countries of the EU. They are currently being replaced by more effective and more tolerable agents such C1-inhibitors, the kallikrein inhibitor ecallantide, and the B2 receptor antagonist icatibant, which have recently obtained market authorization. These new drugs have had a major impact, especially on the indications and procedures for long-term prophylaxis. According to the most recent international consensus papers and our own experience, self-administered C1-inhibitors are now the first option for long-term prophylactic therapy. The decision for prophylaxis should no longer be based on single parameters such as the frequency of attacks but on adequate overall disease control including quality of life. More drugs are currently being developed, which may lead to further changes in the treatment algorithms of HAE.

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Section: Discussionmentioning

confidence: 99%

Prophylaxis in hereditary angioedema (HAE) with C1 inhibitor deficiency

Greve

Straßen

Gorczyza

et al. 2016

J Deutsche Derma Gesell

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“…Andere C1‐INH‐Hersteller evaluieren ebenfalls Rezepturen für die subkutane Langzeitprophylaxe. Biocryst arbeitet an oralen Kallikrein‐Inhibitoren, die Plasma‐Kallikrein hemmen und die Bradykinin‐Produktion unterdrücken . Erste Ergebnisse aus klinischen Studien sind vielversprechend .…”

Section: Ausblickunclassified

Prophylaxe beim hereditären Angioödem (HAE) mit C1‐Inhibitormangel

Greve

Straßen

Gorczyza

et al. 2016

J Deutsche Derma Gesell

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ZusammenfassungDas hereditäre Angioödem (engl.: hereditary angioedema, HAE) ist eine seltene angeborene Erkrankung, die durch wiederkehrende Episoden subkutaner oder submuköser Ödeme charakterisiert ist. Kehlkopf-Manifestationen können lebensbedrohlich sein. In den meisten Fällen kann die Erkrankung mit einem On-Demand-Ansatz angemessen behandelt werden -in einigen Fällen ist jedoch eine Kurz-oder Langzeitprophylaxe angebracht. Attenuierte Androgene waren einmal das Standardmedikament; sie werden jedoch mit erheblichen Nebenwirkungen in Verbindung gebracht und sind in den deutschsprachigen Ländern der EU nicht mehr kommerziell erhältlich. Zurzeit werden sie von wirksameren und besser verträglichen Therapien wie C1-Esterase-Inhibitoren, dem Kallikrein-Inhibitor Ecallantid und dem B2-Rezeptorantagonisten Icatibant verdrängt, welche kürzlich auf dem Markt zugelassen wurden. Diese neuen Medikamente hatten einen erheblichen Einfluss, insbesondere auf die Indikationsstellung und das Vorgehen bei einer Langzeitprophylaxe. Nach den neuesten internationalen Konsenspapieren und unserer eigenen Erfahrung sind selbstverabreichte C1-Inhibitoren nun die erste Option bei der Langzeitprophylaxe. Die Entscheidung für eine Prophylaxe sollte nicht länger auf der Grundlage einzelner Parameter wie der Häufigkeit der Anfälle getroffen werden, sondern auf einer adäquaten allgemeinen Krankheitskontrolle, einschließlich der Lebensqualität. Zurzeit werden weitere Medikamente entwickelt, welche zu weiteren Veränderungen bei den Behandlungsalgorithmen des HAE führen könnten. SummaryHereditary angioedema (HAE) is a rare congenital disorder characterized by recurrent episodes of subcutaneous or submucosal edema. Laryngeal manifestations can be life-threatening. In the majority of cases, the disease can be adequately treated with an on-demand approach -in some cases, however, short-or long-term prophylaxis is indicated. Attenuated androgens used to be the drugs of choice, but they are associated with considerable side effects and no longer commercially available in the German-speaking countries of the EU. They are currently being replaced by more effective and more tolerable agents such C1-inhibitors, the kallikrein inhibitor ecallantide, and the B2 receptor antagonist icatibant, which have recently obtained market authorization. These new drugs have had a major impact, especially on the indications and procedures for long-term prophylaxis. According to the most recent

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“…BCX4161 is an oral small molecule kallikrein inhibitor that is being developed by BioCryst Pharmaceuticals Ltd. (Durham, NC, USA). Preclinical studies showed that it is a potent and specific inhibitor of plasma kallikrein [13]. A Phase IIa proof-of-concept clinical trial (OPuS-1 [Oral ProphylaxiS-1]) of BCX4161 in patients with HAE-C1-INH has been recently initiated [14].…”

Section: New Potential Treatment Options For Hae-c1-inhmentioning

confidence: 99%

Current drugs in early development for hereditary angioedema: potential for effective treatment

Bork

2014

Expert Opinion on Investigational Drugs

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BCX-4161, a Small Molecule and Orally Bioavailable Plasma Kallikrein Inhibitor for the Treatment of Hereditary Angioedema

Cited by 7 publications

References 0 publications

Prophylaxis in hereditary angioedema (HAE) with C1 inhibitor deficiency

Prophylaxis in hereditary angioedema (HAE) with C1 inhibitor deficiency

Prophylaxe beim hereditären Angioödem (HAE) mit C1‐Inhibitormangel

Current drugs in early development for hereditary angioedema: potential for effective treatment

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