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Berotralstat

Cat. No. M11406
Berotralstat  Structure
Size Price Availability
1mg USD 420  USD420 4-7 Days
5mg USD 1240  USD1240 4-7 Days
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Quality Control & Documentation
Biological Activity

Berotralstat (BCX7353) was a second generation plasma kallikrein inhibitor with low toxicity and high specificity, and was used for the diagnosis of hereditary angioedema (HAE). Berotralstat works by blocking the enzyme activity of plasma Kallikrein that releases bradykinin, a major biological peptide that promotes swelling and pain associated with HAE attacks.

Chemical Information
Molecular Weight 562.56
Formula C30H26F4N6O
CAS Number 1809010-50-1
Form Solid
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] No authors listed. Med Lett Drugs Ther. Berotralstat (Orladeyo) for prevention of hereditary angioedema

[2] Michael E Manning, et al. Allergy Asthma Proc. Berotralstat (BCX7353) is a novel oral prophylactic treatment for hereditary angioedema: Review of phase II and III studies

[3] Arnold Lee. Drugs. Berotralstat: First Approval

[4] Isao Ohsawa, et al. Allergy. Oral berotralstat for the prophylaxis of hereditary angioedema attacks in patients in Japan: A phase 3 randomized trial

[5] Bruce Zuraw, et al. J Allergy Clin Immunol. Oral once-daily berotralstat for the prevention of hereditary angioedema attacks: A randomized, double-blind, placebo-controlled phase 3 trial

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