Berotralstat HCl

Catalog No: 20619

CAS Number: 1809010-52-3

Purity: 98% Min.

Berotralstat HCl is a novel selective inhibitor of plasma kallikrein, blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.

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Chemical Information

Name	Berotralstat HCl
Iupac Chemical Name	1-(3-(aminomethyl)phenyl)-N-(5-((3-cyanophenyl)((cyclopropylmethyl)amino)methyl)-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide dihydrochloride
Synonyms	Berotralstat hydrochloride; Berotralstat HCl; Berotralstat dihydrochloride; Berotralstat 2HCl;
Molecular Formula	C30H28Cl2F4N6O
Molecular Weight	635.48
Smile	O=C(C1=CC(C(F)(F)F)=NN1C2=CC=CC(CN)=C2)NC3=CC(C(C4=CC=CC(C#N)=C4)NCC5CC5)=CC=C3F.[H]Cl.[H]Cl
InChiKey	XFZLBLTUANGZBD-UHFFFAOYSA-N
InChi	InChI=1S/C30H26F4N6O.2ClH/c31-24-10-9-22(28(37-17-18-7-8-18)21-5-1-3-19(11-21)15-35)13-25(24)38-29(41)26-14-27(30(32,33)34)39-40(26)23-6-2-4-20(12-23)16-36;;/h1-6,9-14,18,28,37H,7-8,16-17,36H2,(H,38,41);2*1H
CAS Number	1809010-52-3
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Formulation	Solid powder
Purity	98% Min.
Storage	Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility	Soluble in DMSO
Handling
Shipping Condition	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
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Clinical study

1: Mathis A, Sale M, Cornpropst M, Sheridan WP, Ma SC. Population pharmacokinetic modeling and simulations of berotralstat for prophylactic treatment of attacks of hereditary angioedema. Clin Transl Sci. 2022 Apr;15(4):1027-1035. doi: 10.1111/cts.13233. Epub 2022 Feb 25. PMID: 35212456; PMCID: PMC9010267.

2: Gao Y, Hwang J, Hwang G, Craig T. A review of oral kallikrein inhibitor berotralstat for hereditary angioedema. Drugs Today (Barc). 2022 Feb;58(2):59-67. doi: 10.1358/dot.2022.58.2.3369191. PMID: 35188140.

3: Anderson J, Maina N. Reviewing clinical considerations and guideline recommendations of C1 inhibitor prophylaxis for hereditary angioedema. Clin Transl Allergy. 2022 Jan 18;12(1):e12092. doi: 10.1002/clt2.12092. PMID: 35079346; PMCID: PMC8764638.

4: Kelbel T. A case of normal C1 esterase inhibitor hereditary angioedema successfully treated with berotralstat. Ann Allergy Asthma Immunol. 2022 Apr;128(4):462-463. doi: 10.1016/j.anai.2022.01.014. Epub 2022 Jan 19. PMID: 35063629.

5: Soteres DF, Grimes F. Patient and caregiver perspectives on transitioning to oral prophylaxis in the emerging hereditary angioedema treatment landscape. Clin Case Rep. 2021 Nov 16;9(11):e05086. doi: 10.1002/ccr3.5086. PMID: 34815876; PMCID: PMC8593787.

6: Orui S, Nozue H, Kobayashi S, Fujioka M, Maekawa Y. [Pharmacological and clinical study results of Berotralstat Hydrochloride for long-term prophylactic treatment of hereditary angioedema]. Nihon Yakurigaku Zasshi. 2021;156(6):382-390. Japanese. doi: 10.1254/fpj.21069. PMID: 34719573.

7: Geng B, Craig TJ. Small molecule drugs for atopic dermatitis, rheumatoid arthritis, and hereditary angioedema. Ann Allergy Asthma Immunol. 2022 Mar;128(3):263-268. doi: 10.1016/j.anai.2021.10.015. Epub 2021 Oct 18. PMID: 34673223.

8: Gower RG, Wilber M. Considerations for transition from subcutaneous to oral prophylaxis in the treatment of hereditary angioedema. Allergy Asthma Clin Immunol. 2021 Oct 9;17(1):100. doi: 10.1186/s13223-021-00603-9. PMID: 34627358; PMCID: PMC8501591.

9: Berotralstat (Orladeyo) for prevention of hereditary angioedema. Med Lett Drugs Ther. 2021 Jul 26;63(1629):e7-e8. PMID: 34544111.

10: Manning ME. Recognition and Management of Hereditary Angioedema: Best Practices for Dermatologists. Dermatol Ther (Heidelb). 2021 Oct;11(5):1829-1838. doi: 10.1007/s13555-021-00593-x. Epub 2021 Aug 30. PMID: 34460082; PMCID: PMC8484417.

11: Kotian PL, Wu M, Vadlakonda S, Chintareddy V, Lu P, Juarez L, Kellogg-Yelder D, Chen X, Muppa S, Chambers-Wilson R, Davis Parker C, Williams J, Polach KJ, Zhang W, Raman K, Babu YS. Berotralstat (BCX7353): Structure-Guided Design of a Potent, Selective, and Oral Plasma Kallikrein Inhibitor to Prevent Attacks of Hereditary Angioedema (HAE). J Med Chem. 2021 Sep 9;64(17):12453-12468. doi: 10.1021/acs.jmedchem.1c00511. Epub 2021 Aug 26. PMID: 34436898.

12: Powell J, Piszczatoski C, Rubido E. Orladeyo (Berotralstat): A Novel Oral Therapy for the Prevention of Hereditary Angioedema. Ann Pharmacother. 2022 Apr;56(4):488-493. doi: 10.1177/10600280211032982. Epub 2021 Jul 20. PMID: 34282650.

13: Farkas H, Stobiecki M, Peter J, Kinaciyan T, Maurer M, Aygören-Pürsün E, Kiani-Alikhan S, Wu A, Reshef A, Bygum A, Fain O, Hagin D, Huissoon A, Jeseňák M, Lindsay K, Panovska VG, Steiner UC, Zubrinich C, Best JM, Cornpropst M, Dix D, Dobo SM, Iocca HA, Desai B, Murray SC, Nagy E, Sheridan WP. Long-term safety and effectiveness of berotralstat for hereditary angioedema: The open-label APeX-S study. Clin Transl Allergy. 2021 Jun;11(4):e12035. doi: 10.1002/clt2.12035. PMID: 34161665; PMCID: PMC8221587.

14: Manning ME, Kashkin JM. Berotralstat (BCX7353) is a novel oral prophylactic treatment for hereditary angioedema: Review of phase II and III studies. Allergy Asthma Proc. 2021 Jul 14;42(4):274-282. doi: 10.2500/aap.2021.42.210034. Epub 2021 Jun 14. PMID: 34127176.

15: Arruda LK, Ferriani MPL. Treatment of hereditary angioedema: When the goal is having a normal life. J Allergy Clin Immunol. 2021 Jul;148(1):80-82. doi: 10.1016/j.jaci.2021.05.023. Epub 2021 May 28. PMID: 34058236.

16: Wedner HJ, Aygören-Pürsün E, Bernstein J, Craig T, Gower R, Jacobs JS, Johnston DT, Lumry WR, Zuraw BL, Best JM, Iocca HA, Murray SC, Desai B, Nagy E, Sheridan WP, Kiani-Alikhan S. Randomized Trial of the Efficacy and Safety of Berotralstat (BCX7353) as an Oral Prophylactic Therapy for Hereditary Angioedema: Results of APeX-2 Through 48 Weeks (Part 2). J Allergy Clin Immunol Pract. 2021 Jun;9(6):2305-2314.e4. doi: 10.1016/j.jaip.2021.03.057. Epub 2021 Apr 15. PMID: 33866032.

17: Lee A. Berotralstat: First Approval. Drugs. 2021 Feb;81(3):405-409. doi: 10.1007/s40265-021-01475-4. PMID: 33646555.

18: Ohsawa I, Honda D, Suzuki Y, Fukuda T, Kohga K, Morita E, Moriwaki S, Ishikawa O, Sasaki Y, Tago M, Chittick G, Cornpropst M, Murray SC, Dobo SM, Nagy E, Van Dyke S, Reese L, Best JM, Iocca H, Collis P, Sheridan WP, Hide M. Oral berotralstat for the prophylaxis of hereditary angioedema attacks in patients in Japan: A phase 3 randomized trial. Allergy. 2021 Jun;76(6):1789-1799. doi: 10.1111/all.14670. Epub 2020 Dec 23. PMID: 33247955; PMCID: PMC8247297.

19: Zuraw B, Lumry WR, Johnston DT, Aygören-Pürsün E, Banerji A, Bernstein JA, Christiansen SC, Jacobs JS, Sitz KV, Gower RG, Gagnon R, Wedner HJ, Kinaciyan T, Hakl R, Hanzlíková J, Anderson JT, McNeil DL, Fritz SB, Yang WH, Tachdjian R, Busse PJ, Craig TJ, Li HH, Farkas H, Best JM, Clemons D, Cornpropst M, Dobo SM, Iocca HA, Kargl D, Nagy E, Murray SC, Collis P, Sheridan WP, Maurer M, Riedl MA. Oral once-daily berotralstat for the prevention of hereditary angioedema attacks: A randomized, double-blind, placebo-controlled phase 3 trial. J Allergy Clin Immunol. 2021 Jul;148(1):164-172.e9. doi: 10.1016/j.jaci.2020.10.015. Epub 2020 Oct 21. PMID: 33098856.

20: Hwang JR, Hwang G, Johri A, Craig T. Oral plasma kallikrein inhibitor BCX7353 for treatment of hereditary angioedema. Immunotherapy. 2019 Dec;11(17):1439-1444. doi: 10.2217/imt-2019-0128. Epub 2019 Oct 22. PMID: 31635497.

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20619 - Berotralstat HCl | CAS 1809010-52-3

Berotralstat HCl

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