Peringatan Keamanan

The intraperitoneal LD50 of abametapir in mice is 225 mg/kg.L15158 Topical formulations of abametapir contain benzyl alcohol, which has been associated with fatal reactions including "gasping syndrome" following systemic exposure in neonates and low birth weight infants. The use of benzyl alcohol-containing abametapir formulations should be avoided in patients <6 months of age due to an increased risk of unintentional systemic absorption.L15153 As benzyl alcohol toxicity may also occur in pediatric patients following accidental oral ingestion, the manufacturer recommends that it be administered to pediatric patients only under the direct supervision of adult.L15153 Symptoms of benzyl alcohol toxicity may include significant gastrointestinal and central nervous system adverse effects, with severe cases leading to respiratory depression and death.L15153 If toxicity is expected, patients should be advised to contact their nearest poison control center.

The minimal amount of benzyl alcohol at which toxicity might occur is unclear. Toxicity is more likely in premature infants, low birth weight infants, and those receiving high doses.L15153

Abametapir

DB11932

small molecule approved investigational

Deskripsi

Abametapir is a novel pediculicidal metalloproteinase inhibitor used to treat infestations of head lice.L15153 The life cycle of head lice (Pediculus capitis) is approximately 30 days, seven to twelve of which are spent as eggs laid on hair shafts near the scalp.A216183 Topical pediculicides generally lack adequate ovicidal activity,A216183 including standard-of-care treatments such as permethrin, and many require a second administration 7-10 days following the first to kill newly hatched lice that resisted the initial treatment. The necessity for follow-up treatment may lead to challenges with patient adherence, and resistance to agents like permethrin and pyrethrins/piperonyl butoxide may be significant in some areas.A216228

Investigations into novel ovicidal treatments revealed that several metalloproteinase enzymes were critical to the egg hatching and survival of head lice, and these enzymes were therefore identified as a potential therapeutic target.A216178 Abemetapir is an inhibitor of these metalloproteinase enzymes, and the first topical pediculicide to take advantage of this novel target. The improved ovicidal activity (90-100% in vitro) of abemetapir allows for a single administration, in contrast to many other topical treatments, and its novel and relatively non-specific mechanism may help to curb the development of resistance to this agent.A216178

Abametapir was first approved for use in the United States under the brand name Xeglyze on July 27, 2020.L15163

Struktur Molekul 2D

Berat 184.242
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-lives of abametapir and its metabolites have not been well-characterized, but the estimated half-life of abametapir carboxyl is 71 ± 40 hours (or longer) in adults.[L15153]
Volume Distribusi Data regarding the volume of distribution of abametapir are not available.
Klirens (Clearance) The clearance and excretion of abametapir has not been examined in patients.[L15153]

Absorpsi

In a pharmacokinetic trial with both adult and pediatric patients, the Cmax and AUC0-8h in the adult group were 41 ng/mL and 121 ng.h/mL and the Cmax and AUC0-8h in the pediatric group were 73 ng/mL and 264 ng.h/mL.L15153 In general, systemic exposure to abametapir appears to decrease with increasing age.L15153 The median Tmax of abemetapir is 0.57 - 1.54 hours.L15153 Following topical administration, benzyl alcohol was found in detectable quantities in the serum of 7 out of 39 pediatric patients. The Cmax of benzyl alcohol in these subjects ranged from 0.52 to 3.57 ?g/mL.L15153 The predominant circulating metabolite of abemetapir (abemtapir carboxylate) is eliminated slowly from the circulation and is therefore found at higher serum concentrations than its parent drug - based on data collected for 72 hours post-administration, the ratios of serum Cmax and AUC0-72h between abametapir and abametapir carboxylate were approximately 30 and 250, respectively.L15153

Metabolisme

The biotransformation of abametapir is extensive and primarily mediated by CYP1A2. It is metabolized first to abametapir hydroxyl and then further to abametapir carboxyl - the latter is cleared slowly from the plasma, resulting in higher systemic concentrations than that of the parent drug.L15153 In vitro studies suggest that abametapir carboxyl may act as an inhibitor of CYP3A4, CYP2B6, and CYP1A2, particularly at the relatively high and prolonged concentrations observed following topical administration of abametapir.L15153

Rute Eliminasi

The clearance and excretion of abametapir has not been examined in patients.L15153

Interaksi Obat

889 Data
Eliglustat The serum concentration of Eliglustat can be increased when it is combined with Abametapir.
Ibrutinib The serum concentration of Ibrutinib can be increased when it is combined with Abametapir.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Abametapir.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Abametapir.
Iloperidone The serum concentration of Iloperidone can be increased when it is combined with Abametapir.
Retapamulin The serum concentration of Retapamulin can be increased when it is combined with Abametapir.
Tofacitinib The serum concentration of Tofacitinib can be increased when it is combined with Abametapir.
Vardenafil The serum concentration of Vardenafil can be increased when it is combined with Abametapir.
Eszopiclone The serum concentration of Eszopiclone can be increased when it is combined with Abametapir.
Zopiclone The serum concentration of Zopiclone can be increased when it is combined with Abametapir.
Lovastatin The serum concentration of Lovastatin can be increased when it is combined with Abametapir.
Alfuzosin The serum concentration of Alfuzosin can be increased when it is combined with Abametapir.
Alprazolam The serum concentration of Alprazolam can be increased when it is combined with Abametapir.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Abametapir.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Abametapir.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Abametapir.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Abametapir.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Abametapir.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Abametapir.
Atorvastatin The serum concentration of Atorvastatin can be increased when it is combined with Abametapir.
Aripiprazole The serum concentration of Aripiprazole can be increased when it is combined with Abametapir.
Aripiprazole lauroxil The serum concentration of Aripiprazole lauroxil can be increased when it is combined with Abametapir.
Phentermine The serum concentration of Phentermine can be increased when it is combined with Abametapir.
Azithromycin The serum concentration of Azithromycin can be increased when it is combined with Abametapir.
Ziprasidone The serum concentration of Ziprasidone can be increased when it is combined with Abametapir.
Methysergide The serum concentration of Methysergide can be increased when it is combined with Abametapir.
Terfenadine The serum concentration of Terfenadine can be increased when it is combined with Abametapir.
Prochlorperazine The serum concentration of Prochlorperazine can be increased when it is combined with Abametapir.
Meperidine The serum concentration of Meperidine can be increased when it is combined with Abametapir.
Chlorpromazine The serum concentration of Chlorpromazine can be increased when it is combined with Abametapir.
Albendazole The serum concentration of Albendazole can be increased when it is combined with Abametapir.
Cephalexin The serum concentration of Cephalexin can be increased when it is combined with Abametapir.
Doxazosin The serum concentration of Doxazosin can be increased when it is combined with Abametapir.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Abametapir.
Astemizole The serum concentration of Astemizole can be increased when it is combined with Abametapir.
Norethisterone The serum concentration of Norethisterone can be increased when it is combined with Abametapir.
Fenofibrate The serum concentration of Fenofibrate can be increased when it is combined with Abametapir.
Atazanavir The serum concentration of Atazanavir can be increased when it is combined with Abametapir.
Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Abametapir.
Pimozide The serum concentration of Pimozide can be increased when it is combined with Abametapir.
Amiodarone The serum concentration of Amiodarone can be increased when it is combined with Abametapir.
Fosphenytoin The serum concentration of Fosphenytoin can be increased when it is combined with Abametapir.
St. John's Wort The serum concentration of St. John's Wort can be increased when it is combined with Abametapir.
Drospirenone The serum concentration of Drospirenone can be increased when it is combined with Abametapir.
Pranlukast The serum concentration of Pranlukast can be increased when it is combined with Abametapir.
Allylestrenol The serum concentration of Allylestrenol can be increased when it is combined with Abametapir.
Zuclopenthixol The serum concentration of Zuclopenthixol can be increased when it is combined with Abametapir.
Roflumilast The serum concentration of Roflumilast can be increased when it is combined with Abametapir.
Cobimetinib The serum concentration of Cobimetinib can be increased when it is combined with Abametapir.
Lacosamide The serum concentration of Lacosamide can be increased when it is combined with Abametapir.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Abametapir.
Fosaprepitant The serum concentration of Fosaprepitant can be increased when it is combined with Abametapir.
Lomitapide The serum concentration of Lomitapide can be increased when it is combined with Abametapir.
Linagliptin The serum concentration of Linagliptin can be increased when it is combined with Abametapir.
Vorapaxar The serum concentration of Vorapaxar can be increased when it is combined with Abametapir.
Suvorexant The serum concentration of Suvorexant can be increased when it is combined with Abametapir.
Netupitant The serum concentration of Netupitant can be increased when it is combined with Abametapir.
Idelalisib The serum concentration of Idelalisib can be increased when it is combined with Abametapir.
Ceritinib The serum concentration of Ceritinib can be increased when it is combined with Abametapir.
Tasimelteon The serum concentration of Tasimelteon can be increased when it is combined with Abametapir.
Nintedanib The serum concentration of Nintedanib can be increased when it is combined with Abametapir.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Abametapir.
Osimertinib The serum concentration of Osimertinib can be increased when it is combined with Abametapir.
Vitamin D The serum concentration of Vitamin D can be increased when it is combined with Abametapir.
Dihydroergocornine The serum concentration of Dihydroergocornine can be increased when it is combined with Abametapir.
Isavuconazole The serum concentration of Isavuconazole can be increased when it is combined with Abametapir.
Ribociclib The serum concentration of Ribociclib can be increased when it is combined with Abametapir.
Ebastine The serum concentration of Ebastine can be increased when it is combined with Abametapir.
Duvelisib The serum concentration of Duvelisib can be increased when it is combined with Abametapir.
Dacomitinib The serum concentration of Dacomitinib can be increased when it is combined with Abametapir.
Alpelisib The serum concentration of Alpelisib can be increased when it is combined with Abametapir.
Gilteritinib The serum concentration of Gilteritinib can be increased when it is combined with Abametapir.
Siponimod The serum concentration of Siponimod can be increased when it is combined with Abametapir.
9-aminocamptothecin The serum concentration of 9-aminocamptothecin can be increased when it is combined with Abametapir.
Lefamulin The serum concentration of Lefamulin can be increased when it is combined with Abametapir.
Tazemetostat The serum concentration of Tazemetostat can be increased when it is combined with Abametapir.
Methylprednisone The serum concentration of Methylprednisone can be increased when it is combined with Abametapir.
Dihydroergocristine The serum concentration of Dihydroergocristine can be increased when it is combined with Abametapir.
Dihydroergocryptine The serum concentration of Dihydroergocryptine can be increased when it is combined with Abametapir.
Medical Cannabis The serum concentration of Medical Cannabis can be increased when it is combined with Abametapir.
Elexacaftor The serum concentration of Elexacaftor can be increased when it is combined with Abametapir.
Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Abametapir.
Bortezomib The serum concentration of Bortezomib can be increased when it is combined with Abametapir.
Dofetilide The serum concentration of Dofetilide can be increased when it is combined with Abametapir.
Cabergoline The serum concentration of Cabergoline can be increased when it is combined with Abametapir.
Theophylline The serum concentration of Theophylline can be increased when it is combined with Abametapir.
Vindesine The serum concentration of Vindesine can be increased when it is combined with Abametapir.
Vinorelbine The serum concentration of Vinorelbine can be increased when it is combined with Abametapir.
Clozapine The serum concentration of Clozapine can be increased when it is combined with Abametapir.
Sorafenib The serum concentration of Sorafenib can be increased when it is combined with Abametapir.
Teniposide The serum concentration of Teniposide can be increased when it is combined with Abametapir.
Erlotinib The serum concentration of Erlotinib can be increased when it is combined with Abametapir.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Abametapir.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Abametapir.
Carbamazepine The serum concentration of Carbamazepine can be increased when it is combined with Abametapir.
Vinblastine The serum concentration of Vinblastine can be increased when it is combined with Abametapir.
Imatinib The serum concentration of Imatinib can be increased when it is combined with Abametapir.
Tamoxifen The serum concentration of Tamoxifen can be increased when it is combined with Abametapir.
Etoposide The serum concentration of Etoposide can be increased when it is combined with Abametapir.
Sirolimus The serum concentration of Sirolimus can be increased when it is combined with Abametapir.

Referensi & Sumber

Synthesis reference: Ronald Harding, Lewis David Schulz, Vernon Morrison Bowles, "Pediculicidal composition." WIPO Patent WO2015107384A2, published July, 2015.
Artikel (PubMed)
  • PMID: 28082644
    Bowles VM, Yoon KS, Barker SC, Tran C, Rhodes C, Clark MJ: Ovicidal Efficacy of Abametapir Against Eggs of Human Head and Body Lice (Anoplura: Pediculidae). J Med Entomol. 2017 Jan;54(1):167-172. doi: 10.1093/jme/tjw132. Epub 2016 Aug 21.
  • PMID: 30828591
    Bowles VM, Hanegraaf S, Ahveninen T, Sidgiddi S, Allenby K, Alsop H: Effect of a New Head Lice Treatment, Abametapir Lotion, 0.74%, on Louse Eggs: A Randomized, Double-Blind Study. Glob Pediatr Health. 2019 Feb 22;6:2333794X19831295. doi: 10.1177/2333794X19831295. eCollection 2019.
  • PMID: 31083883
    Gunning K, Kiraly B, Pippitt K: Lice and Scabies: Treatment Update. Am Fam Physician. 2019 May 15;99(10):635-642.

Contoh Produk & Brand

Produk: 1 • International brands: 1
Produk
  • Xeglyze
    Lotion • 0.74 g/100g • Topical • US • Approved
International Brands
  • Xeglyze

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