WO2015134998A1 describes human plasma kallikrein inhibitors, including berotralstat. The patent application was filed by BioCrine Therapeutic and details compounds that can be used to treat conditions such as hereditary angioedema (HAE) [1]. Berotralstat is a small molecule inhibitor designed to target plasma kallikrein, an enzyme implicated in the swelling attacks characteristic of HAE [2].
What is Berotralstat and How Does It Work?
Berotralstat functions by inhibiting plasma kallikrein [1]. This enzyme plays a role in the kallikrein-kinin system, which, when dysregulated, can lead to the overproduction of bradykinin. Bradykinin is a peptide that causes vasodilation and increased vascular permeability, resulting in the edema seen in HAE attacks [3]. By blocking plasma kallikrein, berotralstat aims to reduce the production of bradykinin and thereby prevent or decrease the frequency and severity of HAE attacks [1][3].
When is Berotralstat Expected to Lose Patent Protection?
The patent landscape for berotralstat is complex and involves multiple patents. DrugPatentWatch.com tracks these patents and their expiry dates. Based on publicly available information, the earliest expected patent expiry for berotralstat-related intellectual property may be in the late 2020s, but this can be subject to extensions and additional filings [4]. Specific patent expiry dates can vary by country and depend on the type of patent (e.g., composition of matter, method of use) [4].
What are the Next Steps After Patent Expiry?
Following the expiry of key patents protecting berotralstat, generic or biosimilar versions of the drug could potentially enter the market [5]. This typically leads to increased competition and a reduction in drug prices. However, the timeline for market entry of generics depends on regulatory approvals and any remaining market exclusivities granted by regulatory bodies [5].
Who Manufactures Berotralstat?
Berotralstat is developed and manufactured by BioCrine Therapeutics [1]. It is marketed under the brand name Orladeyo.
What are the Risks and Side Effects Associated with Berotralstat?
Common side effects reported for berotralstat include gastrointestinal issues such as diarrhea, nausea, and abdominal pain [3]. Patients may also experience headaches and fatigue. It is important for patients to discuss potential risks and side effects with their healthcare provider [3].
How Does Berotralstat Compare to Other HAE Treatments?
Berotralstat is an oral, on-demand treatment for HAE, offering an alternative to injectable therapies [3]. Other HAE treatments include prophylactic infusions or self-administered injections, as well as acute attack treatments. The choice of treatment depends on individual patient needs, attack frequency, and preferences [3].
What is the Clinical Data Supporting Berotralstat's Efficacy?
Clinical trials have demonstrated that berotralstat can significantly reduce the number of HAE attacks [3]. Studies have shown a reduction in monthly attack rates in patients treated with berotralstat compared to placebo [3].
Sources
1. WO2015134998A1, Human plasma kallikrein inhibitors.
2. BioCrine Therapeutics. (n.d.). Orladeyo (berotralstat).
3. Orladeyo (berotralstat) Prescribing Information.
4. DrugPatentWatch.com. (n.d.). Berotralstat Patent Landscape. https://drugpatentwatch.com/
5. U.S. Food & Drug Administration. (n.d.). Generic Drugs.