Camostat Explained

Verifiedrevid:443459490
Iupac Name:N,N-Dimethylcarbamoylmethyl 4-(4-guanidinobenzoyloxy)phenylacetate
Tradename:Foipan
Synonyms:FOY-305
Legal Us:Not FDA approved
Legal Status:Rx-only
Routes Of Administration:Oral
Iuphar Ligand:6432
Cas Number:59721-28-7
Atc Prefix:B02
Atc Suffix:AB04
Pubchem:2536
Chemspiderid:2440
Chebi:135632
Unii:0FD207WKDU
Kegg:D07606
Chembl:590799
C:20
H:22
N:4
O:5
Smiles:CN(C)C(=O)COC(=O)CC1=CC=C(C=C1)OC(=O)C2=CC=C(C=C2)N=C(N)N
Stdinchi:1S/C20H22N4O5/c1-24(2)17(25)12-28-18(26)11-13-3-9-16(10-4-13)29-19(27)14-5-7-15(8-6-14)23-20(21)22/h3-10H,11-12H2,1-2H3,(H4,21,22,23)
Stdinchikey:XASIMHXSUQUHLV-UHFFFAOYSA-N

Camostat is a serine protease inhibitor. Serine protease enzymes have a variety of functions in the body, and so camostat has a diverse range of uses. Camostat is approved in Japan for the treatment of chronic pancreatitis and postoperative reflux esophagitis.[1] [2] The oral proteolytic enzyme inhibitor has been on the market since 1985 under the trade name Foipan Tablets. The manufacturer is Ono Pharmaceutical. The drug is used in the treatment of some forms of cancer and is also effective against some viral infections, as well as inhibiting fibrosis in liver or kidney disease or pancreatitis.[3] [4] [5] [6] [7]

Pharmacology

It is an inhibitor of the enzyme transmembrane protease, serine 2 (TMPRSS2).For chronic pancreatitis camostat's typical dose is 600 mg daily, for postoperative reflux esophagitis 300 mg are taken. The daily dose is split in 3 doses and taken after each meal.[1] [8]

Side effects

As side effects allergic reactions including anaphylaxis, hypersensitivity, hyperkalemia, platelet and leukocyte depletion, liver dysfunction, jaundice have been reported.[9]

COVID-19

Inhibition of TMPRSS2 partially blocked infection by SARS-CoV and Human coronavirus NL63 in HeLa cell cultures.[10] Another in vitro study showed that camostat significantly reduces the infection of Calu-3 lung cells by SARS-CoV-2, the virus responsible for COVID-19.[11] [12] It is currently in many Phase 1 and Phase 2 clinical trials.[13]

Camostat decreased CRP levels better compared to Lopinavir/Ritonavir in a small study of mild COVID-19 patients.[14] Camostat decreased COVID-19 severity, improved inflammatory markers and oxygenation compared to hydroxychloroquine treated patients.[15]

A study of 205 COVID-19 patients treated with Camostat, carried out at Aarhus University Hospital in Denmark and concluding in April 2021, showed no noticeable effects of Camostat on duration of hospitalisation or severity of the cases, but noted that higher doses (the study used 600 mg Camostat daily dosage) might still have a possible effect.[16]

On July 1, 2021, the AIDS Clinical Trials Group announced that the Camostat group on the "ACTIV-2 Outpatient Monoclonal Antibodies and Other Therapies Trial" would not be moving forward to Phase 3. The trial demonstrated no safety concerns but also no changes in viral shedding or symptom improvement.[17]

External links

Notes and References

  1. Web site: FOIPAN® Tablets 100mg . Ono Pharmaceutical Co., Ltd. .
  2. Web site: Camostat . .
  3. Okuno M, Kojima S, Akita K, Matsushima-Nishiwaki R, Adachi S, Sano T, Takano Y, Takai K, Obora A, Yasuda I, Shiratori Y, Okano Y, Shimada J, Suzuki Y, Muto Y, Moriwaki Y . 6 . Retinoids in liver fibrosis and cancer . Frontiers in Bioscience . 7 . 4 . d204–d218 . January 2002 . 11779708 . 10.2741/A775 .
  4. Hsieh HP, Hsu JT . Strategies of development of antiviral agents directed against influenza virus replication . Current Pharmaceutical Design . 13 . 34 . 3531–3542 . 2007 . 18220789 . 10.2174/138161207782794248 .
  5. Kitamura K, Tomita K . Proteolytic activation of the epithelial sodium channel and therapeutic application of a serine protease inhibitor for the treatment of salt-sensitive hypertension . Clinical and Experimental Nephrology . 16 . 1 . 44–48 . February 2012 . 22038264 . 10.1007/s10157-011-0506-1 . 6522071 .
  6. Zhou Y, Vedantham P, Lu K, Agudelo J, Carrion R, Nunneley JW, Barnard D, Pöhlmann S, McKerrow JH, Renslo AR, Simmons G . 6 . Protease inhibitors targeting coronavirus and filovirus entry . Antiviral Research . 116 . 76–84 . April 2015 . 25666761 . 4774534 . 10.1016/j.antiviral.2015.01.011 .
  7. Ueda M, Uchimura K, Narita Y, Miyasato Y, Mizumoto T, Morinaga J, Hayata M, Kakizoe Y, Adachi M, Miyoshi T, Shiraishi N, Kadowaki D, Sakai Y, Mukoyama M, Kitamura K . 6 . The serine protease inhibitor camostat mesilate attenuates the progression of chronic kidney disease through its antioxidant effects . Nephron . 129 . 3 . 223–232 . 2015 . 25766432 . 10.1159/000375308 . 207652863 .
  8. Breining P, Frølund AL, Højen JF, Gunst JD, Staerke NB, Saedder E, Cases-Thomas M, Little P, Nielsen LP, Søgaard OS, Kjolby M . Camostat mesylate against SARS-CoV-2 and COVID-19-Rationale, dosing and safety . Basic & Clinical Pharmacology & Toxicology . 128 . 2 . 204–212 . February 2021 . 33176395 . 10.1111/bcpt.13533. free .
  9. Web site: 医療用医薬品 : カモスタットメシル酸塩 (カモスタットメシル酸塩錠100mg「日医工」) . KEGG . ja . 2021-02-05.
  10. Kawase M, Shirato K, van der Hoek L, Taguchi F, Matsuyama S . Simultaneous treatment of human bronchial epithelial cells with serine and cysteine protease inhibitors prevents severe acute respiratory syndrome coronavirus entry . Journal of Virology . 86 . 12 . 6537–6545 . June 2012 . 22496216 . 3393535 . 10.1128/JVI.00094-12 .
  11. Hoffmann M, Kleine-Weber H, Schroeder S, Krüger N, Herrler T, Erichsen S, Schiergens TS, Herrler G, Wu NH, Nitsche A, Müller MA, Drosten C, Pöhlmann S . 6 . SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor . Cell . 181 . 2 . 271–280.e8 . April 2020 . 32142651 . 7102627 . 10.1016/j.cell.2020.02.052 .
  12. Jackson CB, Farzan M, Chen B, Choe H . Mechanisms of SARS-CoV-2 entry into cells . Nature Reviews. Molecular Cell Biology . 23 . 1 . 3–20 . January 2022 . 34611326 . 8491763 . 10.1038/s41580-021-00418-x .
  13. Web site: Search of: camostat - covid - List Results . ClinicalTrials.gov . 2021-02-04.
  14. Choi JP, Kim HJ, Han J, Park S, Han J . Foistar(Camostat mesylate) associated with the significant decrease in CRP levels compared to Kaletra(Lopinavir/Ritonavir) treatment in Korean mild COVID-19 pneumonic patients. . 2020-12-15 . Infectious Diseases (except HIV/AIDS) . 10.1101/2020.12.10.20240689 . en .
  15. Hofmann-Winkler H, Moerer O, Alt-Epping S, Bräuer A, Büttner B, Müller M, Fricke T, Grundmann J, Harnisch LO, Heise D, Kernchen A, Pressler M, Stephani C, Tampe B, Kaul A, Gärtner S, Kramer S, Pöhlmann S, Winkler MS . 6 . Camostat Mesylate May Reduce Severity of Coronavirus Disease 2019 Sepsis: A First Observation . Critical Care Explorations . 2 . 11 . e0284 . November 2020 . 33225308 . 7671878 . 10.1097/CCE.0000000000000284 . 20.500.11850/460814 .
  16. Web site: Middel mod halsbrand bremsede ikke Covid-19. 2021-04-28. newsroom.au.dk. da.
  17. Web site: ACTG announces Camostat will not advance to phase 3 in outpatient treatment study for COVID-19. 2021-07-01. EurekAlert!. en.

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