Berotralstat
Berotralstat is an oral plasma kallikrein inhibitor used to prevent attacks of hereditary angioedema (HAE) in adults and children as young as 2 years old.
🧬 Where this information comes from Click to expand
The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 1 clinical label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →
📖 Berotralstat: Patient Information Guide
A plain-language walkthrough of Berotralstat — what it treats, how it works, how it’s taken, side effects, warnings and interactions. Tap any section to expand it.
🎯What it's used for▾
Berotralstat is used specifically to prevent attacks of hereditary angioedema (HAE). Here is the full picture of its approved uses:
- Orladeyo (berotralstat) is indicated for the prevention (prophylaxis) of HAE attacks in adults and pediatric patients 2 years of age and older.
- Orladeyo capsules are approved for adults and children aged 12 and older.
- Orladeyo oral pellets are approved for children aged 2 to less than 12 years, with dosing based on the child's body weight.
- Orladeyo is not approved to treat an acute (active) HAE attack — it has not been shown to be safe or effective for that purpose.
⚙️How it works▾
In people with HAE, a protein called C1-inhibitor is deficient or not working properly. This allows an enzyme called plasma kallikrein to run unchecked. When plasma kallikrein is overactive, it breaks down another protein (called high-molecular-weight kininogen) to produce bradykinin — a potent chemical that makes blood vessel walls leaky, causing the swelling and pain of an HAE attack. Berotralstat works by tightly binding to plasma kallikrein and blocking its activity, which keeps bradykinin production under control and reduces how often attacks occur.
💊How it's taken▾
Orladeyo is taken by mouth once a day with food. Adults and children 12 and older use the capsule form. Children aged 2 to under 12 use the oral pellet packets, with the dose determined by the child's weight.
- Orladeyo capsules: once daily with a meal.
- Orladeyo oral pellets: once daily; a meal should be eaten just before or right after the dose. Pellets can be swallowed with a non-acidic drink or sprinkled on a small amount of soft, non-acidic food — consume within 10 minutes.
- People with moderate or severe liver impairment may need a dose adjustment (capsule form only for adults and patients 12+); children 2 to under 12 with moderate or severe liver impairment should not use Orladeyo.
- Never take extra doses to prevent an attack or make up for a missed one — always follow your prescriber's instructions.
🤒Side effects — in detail▾
The most common side effects of Orladeyo — seen in at least 10% of patients — tend to show up early in treatment and usually improve over time:
- Abdominal (stomach) pain or discomfort
- Vomiting
- Diarrhea
- Back pain
- Gastroesophageal reflux disease (GERD — stomach acid coming up into the esophagus)
Gut-related side effects were more common at higher doses but typically became less frequent as treatment continued. More rarely, some patients had elevated liver enzymes on blood tests. If stomach side effects persist, contact your doctor — a dose adjustment may help.
⚠️Warnings & precautions▾
- Do not take extra doses or go above the prescribed amount. At doses higher than recommended, berotralstat can prolong the QTc interval — an electrical measurement of the heart's rhythm. A prolonged QTc can, in serious cases, lead to dangerous irregular heartbeats. This risk increases as the drug level in your blood rises.
- Orladeyo will not stop an attack in progress. Always keep a separate rescue medication available for acute HAE attacks.
- A small number of patients developed elevated liver enzymes during treatment. Your doctor may monitor your liver function with blood tests.
🔀What it interacts with▾
Berotralstat can affect — and be affected by — several types of medications. Key interactions to know about:
- P-gp inducers (e.g., certain seizure medications, rifampin): can significantly lower berotralstat levels in the blood, reducing its effectiveness. Avoid combining with Orladeyo.
- CYP2D6 substrates (many antidepressants, some heart medications, codeine): Orladeyo can raise blood levels of these drugs, increasing their side effects. Your doctor may need to lower the dose of the other medication.
- CYP3A4 substrates (many common medications, including some statins, certain anxiety or immunosuppressant drugs): same concern — Orladeyo can increase their levels. Monitor closely or adjust dosing.
- Desogestrel (a hormonal contraceptive): Orladeyo raises levels of its active form in the body. Discuss risks and benefits with your doctor.
- P-gp substrates (certain heart, cancer, or seizure drugs): at higher-than-recommended doses, Orladeyo can increase their levels. This is another reason never to exceed the prescribed dose.
This is not a complete list of interactions. Always talk with your doctor or pharmacist before starting, stopping, or changing any medication.
📋Before taking it▾
- Tell your doctor about every medication, supplement, and herbal product you take before starting Orladeyo — the interaction list is significant.
- Liver disease: Moderate or severe liver impairment requires a dose reduction (capsules, adults and teens 12+); children 2 to under 12 with moderate or severe liver impairment should not use Orladeyo.
- Kidney disease: Orladeyo is not recommended for patients with end-stage renal disease. Children aged 2 to under 12 with severe kidney impairment should avoid Orladeyo.
- Pregnancy: There is limited human safety data. Animal studies did not show birth defects, but discuss the potential risks with your doctor before using Orladeyo during pregnancy.
- Breastfeeding: It is unknown whether berotralstat passes into human milk. Small amounts were detected in nursing rat pups. Weigh the benefits of breastfeeding against any potential risk with your doctor.
- Always have an acute HAE rescue treatment available — Orladeyo does not work for attacks that are already happening.
📡Pharmacodynamics — effects in the body▾
Orladeyo produces a concentration-dependent reduction in plasma kallikrein activity — the more drug present, the greater the suppression of this enzyme. This effect has been measured in HAE patients taking the medication once daily. At the maximum recommended adult dose, no clinically meaningful change in the QTc interval (a heart rhythm measurement) was observed, but at three times that dose, a meaningful QTc prolongation was seen — confirming that the heart-rhythm risk is directly tied to how much drug is in the bloodstream.
🔬Pharmacokinetics — how your body processes it▾
After taking Orladeyo with food, berotralstat reaches peak blood levels in about 5 hours on average. It builds up gradually in the body, reaching a stable steady-state level within about 6 to 12 days of daily dosing, with roughly 5-fold accumulation at that point. The drug is very extensively bound to proteins in the blood (about 99%) and has a long half-life — typically around 93 hours, meaning it stays in the body for several days after a dose. Berotralstat is broken down mainly by two liver enzymes (CYP2D6 and CYP3A4), and most of it leaves the body through the stool (about 79%), with only a small amount exiting through urine.
📦How to store it▾
Store at 20°C to 25°C (68°F to 77°F).
📄 Written from Berotralstat’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Every point is grounded in that labeling — nothing is invented. How we use AI →
🩺 Pharmacist Counseling Corner
Quick, plain-English answers to the questions patients ask most about Berotralstat — the kind of thing our pharmacy team would talk through with you at the counter.
What exactly is Orladeyo supposed to do for me? ▾
Can I take Orladeyo to stop an HAE attack that's happening right now? ▾
I've been getting stomach issues since starting Orladeyo. Is that normal, and will it get better? ▾
Does it matter if I take this with or without food? ▾
Are there any medications I should be careful about combining with Orladeyo? ▾
Is it safe to take Orladeyo during pregnancy or while breastfeeding? ▾
Is Berotralstat available over the counter? ▾
When was Berotralstat first available? ▾
Who makes Berotralstat? ▾
💬 Answers drafted from Berotralstat’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Grounded in that labeling — nothing is made up. How we use AI →
🧰 Keep exploring
💊 How Berotralstat comes
Berotralstat is available in 2 forms. Different forms and brands can have different approved uses, doses, schedules, and directions. Follow the instructions for your exact product, and do not switch forms without guidance from your prescriber or pharmacist.
Capsule
How this form is used
- Orladeyo capsules are used to prevent HAE attacks in adults and pediatric patients 12 years of age and older.
- Orladeyo capsules are used at a lower dose for adults and patients 12 and older who have moderate or severe liver impairment.
- Orladeyo capsules may be taken at a lower dose for adults and patients 12 and older who experience persistent stomach or gut side effects.
- Orladeyo capsules are taken orally once daily with food.
- Do not take additional doses or doses higher than prescribed — extra doses increase the risk of a heart rhythm problem.
- Swallow Orladeyo capsules whole; follow your prescriber's instructions for the right dose based on your health.
Other oral form
How this form is used
- Orladeyo oral pellets are used to prevent HAE attacks in pediatric patients aged 2 years to less than 12 years.
- Orladeyo oral pellet dose is based on the child's body weight and is taken once daily.
- Orladeyo oral pellets should not be chewed or crushed — doing so breaks the taste-masking coating and causes a bitter taste.
- Pour the entire contents of one packet directly into the mouth and swallow immediately with a non-acidic liquid such as water or milk, OR sprinkle over about one tablespoon of soft, non-acidic food (such as mashed potatoes, pureed bananas, or pudding) and eat immediately.
- Do not use acidic foods like yogurt or applesauce — they dissolve the coating and make the pellets bitter.
- If pellets are sprinkled on food, they must be consumed within 10 minutes or discarded; a meal should be eaten just before or after giving the pellets.
📊 Berotralstat across the U.S. market
How Berotralstat appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.
FDA-listed product records by dose form (tablet variants merged) — FDA National Drug Code Directory. Record counts are not sales or prescription volume.
Also listed with the FDA, not a patient dose form: Powder (4) — bulk drug substance sold to compounders/manufacturers and multi-item kits. These aren’t counted in the dose-form total above.
Share of FDA-listed product records by manufacturer — FDA National Drug Code Directory. Record counts are not sales or prescription volume.
📈 How widely Berotralstat is used
A general measure of how commonly Berotralstat is prescribed, based on Medicaid — one of the largest public drug programs. The figure below is prescriptions filled in Q1–Q4 2025, summed across every form and brand of the drug.
Think of this as a proxy for how widely Berotralstat is used, drawn from freely available public data. Medicaid is just one program — these numbers don’t include Medicare, other government coverage, or commercial and cash-pay prescriptions, so real-world use is higher than what’s shown here.
How commonly is Berotralstat prescribed? Of the 1,596 medications we measure, Berotralstat ranks #1,284 by Medicaid prescriptions — more than 20% of them.
Utilization by Berotralstat product
Pick a product to see its own Medicaid numbers. Each chip is one clinical product — a specific strength & dosage form as defined by RxNorm — with brand-name and generic versions combined.
berotralstat 150 MG Oral Capsule Most dispensed
Summed across the 1 of 3 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 2467565
berotralstat 110 MG Oral Capsule
Summed across the 1 of 2 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 2467573
Shares are of the Medicaid prescriptions shown here. Product grouping follows RxNorm (the National Library of Medicine’s drug terminology), so “one product” means one strength & dosage form regardless of manufacturer. Dollar figures are gross Medicaid reimbursement before mandatory rebates — rebates (often large, especially for brand-name drugs) are confidential, so actual net cost to Medicaid is lower than shown.
Source: Medicaid State Drug Utilization Data (CMS), aggregated by generic ingredient — summed across every NDC (all brands, strengths, salt forms and dosage forms) of Berotralstat, and across all states and both fee-for-service and managed-care claims. A general popularity signal; it excludes Medicare, commercial insurance and cash prescriptions, so it is not total U.S. use. Based on the 2 of 5 listed Berotralstat NDCs with Medicaid activity.
🔍 Compare Berotralstat products
A representative set of FDA-listed product records for Berotralstat — across manufacturers, strengths, and dosage forms, grouped by form with each product’s manufacturer and how the FDA approved it. The same medicine may be made and packaged by different companies, so a single drug can have many directory entries. (It’s also why a refill can look different — a new shape, color, or box — even though it contains the same medication.)
| Strength | Route | Manufacturer / Labeler | Category ⓘ | Details |
|---|---|---|---|---|
| 💊Capsule | ||||
| 110 mg | Oral | BioCryst Pharmaceuticals, Inc. × 2 listings | NDA | View NDC → |
| 150 mg | Oral | BioCryst Pharmaceuticals, Inc. × 2 listings | NDA | View NDC → |
| 110 mg | Oral | BioCryst Pharmaceuticals Inc. × 2 listings | NDA | View NDC → |
| 150 mg | Oral | BioCryst Pharmaceuticals Inc. × 2 listings | NDA | View NDC → |
| 110 mg | — | Catalent Pharma Solutions, LLC | DRUG FOR FURTHER PROCESSING | View NDC → |
| 150 mg | — | Catalent Pharma Solutions, LLC | DRUG FOR FURTHER PROCESSING | View NDC → |
| 💊Other oral form | ||||
| 72 mg | Oral | BioCryst Pharmaceuticals, Inc. × 2 listings | NDA | View NDC → |
| 96 mg | Oral | BioCryst Pharmaceuticals, Inc. × 2 listings | NDA | View NDC → |
| 108 mg | Oral | BioCryst Pharmaceuticals, Inc. × 2 listings | NDA | View NDC → |
| 132 mg | Oral | BioCryst Pharmaceuticals, Inc. × 2 listings | NDA | View NDC → |
| 💊Bulk drug substance | ||||
| 1 kg/kg | — | Cambrex Charles City, Inc. | BULK INGREDIENT | View NDC → |
| 1 kg/kg | — | Cambrex Karlskoga AB | BULK INGREDIENT | View NDC → |
| 1 kg/kg | — | Corden Pharma Bergamo SpA | BULK INGREDIENT | View NDC → |
| 1 kg/kg | — | Hetero Labs Limited | BULK INGREDIENT | View NDC → |
Showing 22 of 22 products — FDA National Drug Code Directory. See every product, package size and price: browse all 22 Berotralstat NDCs →
📈 What people report — real-world data (FDA FAERS)
After a medicine reaches the market, patients, doctors and drugmakers can send the FDA reports of problems they think may be linked to it. Here’s what’s been reported for Berotralstat — a signal of what to watch for, not proof the drug caused it.
Source: openFDA, from the FDA Adverse Event Reporting System (FAERS). These are voluntary reports — they don’t prove the drug caused the effect, and counts reflect how often something was reported, not how often it actually happens. Reports also often name the very problem the medicine is taken for — a common reason to file one is that the drug didn’t help — so for a pain reliever you may see “pain” high on the list; that points to why the report was filed, not to the drug causing the symptom. This counts every report that lists Berotralstat in any role, so the total runs higher than the FDA’s official dashboard, which counts only cases where the drug is the suspect. For the authoritative figures, see the FDA FAERS Public Dashboard. Always talk to your pharmacist or doctor.
🏛️ The road to your pharmacy
How Berotralstat went from FDA review to the pharmacy shelf — the key milestones in its regulatory journey.
Source: Drugs@FDA.
🚨 Recall history
A recall is when a specific batch of a medicine is pulled from the market — usually a manufacturing issue, not a problem with the drug itself. Class I is most serious, Class III least.
Source: openFDA drug enforcement (recall) reports.
RxNorm Concept Web — From Ingredient to Every Form and Strength
This page starts with one ingredient concept (IN). The branches below show its dose-form concepts (SCDF), then the available clinical drug and strength concepts (SCD). Combination products remain separate concepts with their own pages.
RxCUI 2467540 2 dose forms · 6 strengths
-
Dose form (SCDF) Oral Capsule RxCUI 2467564In current FDA listings -
Dose form (SCDF) Oral Pellet RxCUI 2728873In current FDA listings
Look up RxCUI 2467540 in the RxCUI Atlas →
RxNorm is the U.S. National Library of Medicine’s normalized drug vocabulary. Its concept hierarchy can include forms that are not currently marketed; the status on each branch compares that concept with current FDA listings. RxCUIs identify vocabulary concepts, not individual packages or manufacturers.
📦 Supply & shortage status
Whether Berotralstat is in short supply in the U.S. right now, plus any shortage history the FDA has on record. A shortage usually reflects a manufacturing or demand issue — not a safety problem with the drug.
Source: openFDA, from the FDA Drug Shortages database.
🏷️ Sold under these brand names
🏭 Manufacturers & labelers
RxNorm drug class
Berotralstat belongs to the Plasma Kallikrein Inhibitor class.
Classified by RxNorm RxClass — the U.S. National Library of Medicine's standardized drug-classification service (Established Pharmacologic Class from the FDA, the ATC drug family from the WHO, and mechanism of action). Reference only, not medical advice.
🔬 Where this comes from
Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.
How we combine label and product data
HelloPharmacist combines public FDA and NLM records; we don’t author the underlying clinical facts. We identified 1 FDA-filed SPL label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. The representative label is the starting point for the displayed reference monograph; the 12 largest stored in-scope SPL records, which may include that representative, are compared section by section, and the longest available version of each section is retained. Forms, routes, brands, labelers, product-listed strengths, and product-record counts are aggregated separately from ingredient-matched FDA NDC Directory records; package records listed above are associated with the linked SPL; and the normalized concept hierarchy comes from NLM RxNorm.
For canonical ingredient pages, bounded product-attributed indication and administration excerpts may be added to the AI evidence, and the generator is instructed to preserve available product, brand, route, and form qualifiers instead of treating one label as universal. Where a section is identified as AI-written, its plain-language text is generated from bounded label evidence. New draft drug pages remain in the admin review queue before first publication. BioCryst Pharmaceuticals Inc. is the representative DailyMed label linked for verification and dates; it is not the sole source used for the page.
This is general education, not medical advice — always consult your doctor or pharmacist about your medications and any medical condition. For the exact wording of the linked representative label, view that label on DailyMed; some displayed composite sections may come from other in-scope SPL labels. Learn how we use AI and our data sources & update cadence.