Abametapir

{{Short description|Chemical compound}} {{Use American English|date=July 2020}} {{Use dmy dates|date=July 2020}} {{Infobox drug | type =  | image = Abametapir skeletal.svg | image_class = skin-invert-image | width = 70px | alt = | image2 = | width2 = | alt2 = | caption =

| pronounce = | tradename = Xeglyze | Drugs.com = {{Drugs.com|ppa|abametapir}} | MedlinePlus = | licence_CA =  | licence_EU =  | DailyMedID = Abametapir | licence_US =  | pregnancy_AU =  | pregnancy_AU_comment = | pregnancy_category= | dependency_liability = | addiction_liability = | routes_of_administration = Topical | class = Pediculicide, metalloproteinase inhibitor | ATCvet = | ATC_prefix = P03 | ATC_suffix = AX07 | ATC_supplemental =

| IUPAC_name = 5,5'-dimethyl-2,2'-bipyridine | C = 12 | H = 12 | N = 2 | SMILES = CC1=CN=C(C=C1)C2=NC=C(C=C2)C | StdInChI = 1S/C12H12N2/c1-9-3-5-11(13-7-9)12-6-4-10(2)8-14-12/h3-8H,1-2H3 | StdInChI_comment = | StdInChIKey = PTRATZCAGVBFIQ-UHFFFAOYSA-N | density = | density_notes = | melting_point = | melting_high = | melting_notes = | boiling_point = | boiling_notes = | solubility = | sol_units = | specific_rotation = }}

'''Abametapir''', sold under the brand name '''Xeglyze''', is a medication used for the treatment of head lice infestation in people six months of age and older.<ref name="Xeglyze FDA Label">{{cite web | url=https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/206966lbl.pdf | title=Xeglyze (abametapir) lotion, for topical use | publisher=Dr. Reddy's Laboratories. Inc. | website=U.S. Food and Drug Administration (FDA) | access-date=25 July 2020}}</ref><ref name="FDA snapshot">{{cite web | title=Drug Trial Snapshot: Xeglyze | website=U.S. Food and Drug Administration (FDA) | date=24 July 2020 | url=https://www.fda.gov/drugs/drug-approvals-and-databases/drug-trial-snapshot-xeglyze | archive-url=https://web.archive.org/web/20201022214942/https://www.fda.gov/drugs/drug-approvals-and-databases/drug-trial-snapshot-xeglyze | url-status=dead | archive-date=22 October 2020 | access-date=6 August 2020}} {{PD-notice}}</ref>

The most common side effects include skin redness, rash, skin burning sensation, skin inflammation, vomiting, eye irritation, skin itching, and hair color changes.<ref name="FDA snapshot" />

Abametapir is a metalloproteinase inhibitor.<ref name="Xeglyze FDA Label" /> Abametapir was approved for medical use in the United States in July 2020.<ref name="Xeglyze FDA Label" /><ref>{{cite web | title=Drug Approval Package: Xeglyze | website=U.S. Food and Drug Administration (FDA) | date=21 August 2020 | url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/206966Orig1s000TOC.cfm | archive-url=https://web.archive.org/web/20210228130956/https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/206966Orig1s000TOC.cfm | url-status=dead | archive-date=28 February 2021 | access-date=17 January 2021}}</ref> The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.<ref>{{cite web | title=New Drug Therapy Approvals 2020 | website=U.S. Food and Drug Administration (FDA) | date=31 December 2020 | url=https://www.fda.gov/drugs/new-drugs-fda-cders-new-molecular-entities-and-new-therapeutic-biological-products/new-drug-therapy-approvals-2020 | archive-url=https://web.archive.org/web/20210118011953/https://www.fda.gov/drugs/new-drugs-fda-cders-new-molecular-entities-and-new-therapeutic-biological-products/new-drug-therapy-approvals-2020 | url-status=dead | archive-date=18 January 2021 | access-date=17 January 2021}} {{PD-notice}}</ref>

== Medical uses == Abametapir is indicated for the topical treatment of head lice infestation in people six months of age and older.<ref name="Xeglyze FDA Label" /><ref name="FDA snapshot" />

== Contraindications == Abametapir has no contraindications according to the labeling.<ref name="Drugs.com">Abametapir {{Drugs.com|ppa|abametapir}}. Accessed 6 May 2021.</ref>

== Adverse effects == Common adverse effects are burning skin sensations (in 3% of patients), contact dermatitis (2%), skin redness (4%), rash (3%), and vomiting (2%).<ref name="Drugs.com" />

== Interactions == Abametapir blocks the liver enzymes CYP3A4, CYP2B6 and CYP1A2 ''in vitro''. A single application of the drug may lead to increased blood concentrations of drugs that are metabolized by these enzymes.<ref name="Xeglyze FDA Label" />

== Pharmacology == === Mechanism of action === The drug inhibits enzymes called metalloproteinases. In lice, these enzymes play a role in egg development and survival;<ref name="Xeglyze FDA Label" /> and consequently, blocking them will disrupt the lice's life cycle.

=== Pharmacokinetics === After application to the scalp, part of the substance reaches the bloodstream, where most of it (91.3–92.3%) is bound to plasma proteins. It is metabolized primarily by the liver enzyme CYP1A2 to abametapir hydroxyl and further to abametapir carboxyl (see structure drawings). Abametapir carboxyl has a plasma protein binding of 96.0–97.5% and is the predominant of the three substances in the circulation, having a C<sub>max</sub> 30 times and an area under the curve (AUC) 250 times that of abametapir itself.<ref name="Xeglyze FDA Label" />

The elimination half-life of abametapir is 21 hours. That of abametapir carboxyl is not well known; it is thought to be 71±40 hours or longer. It is not known whether the drug is eliminated via the urine or the faeces.<ref name="Xeglyze FDA Label" />

[[File:Abametapir metabolites.svg|thumb|The drug's metabolites in humans: abametapir hydroxyl (left) and abametapir carboxyl (right)<ref name="Xeglyze FDA Label" />]]

== History == The U.S. Food and Drug Administration (FDA) approved abametapir based on evidence from two identical clinical trials of 699 participants with head lice.<ref name="FDA snapshot" /> The trials were conducted at fourteen sites in the United States.<ref name="FDA snapshot" />

The benefit and side effects of abametapir were evaluated in two clinical trials that enrolled participants with head lice who were at least six months old.<ref name="FDA snapshot" />

About half of all enrolled participants was randomly assigned to abametapir and the other half to placebo.<ref name="FDA snapshot" /> Abametapir lotion or placebo lotion were applied once as a ten-minute treatment to infested hair.<ref name="FDA snapshot" /> The benefit of abametapir in comparison to placebo was assessed after 1, 7 and 14 days by comparing the counts of participants in each group who were free of live lice.<ref name="FDA snapshot" />

== References == {{reflist}}

== Further reading == * {{cite journal |vauthors=Bowles VM, VanLuvanee LJ, Alsop H, Hazan L, Shepherd K, Sidgiddi S, Allenby K, Ahveninen T, Hanegraaf S |title=Clinical studies evaluating abametapir lotion, 0.74%, for the treatment of head louse infestation |journal=Pediatr Dermatol |volume=35 |issue=5 |pages=616–621 |date=September 2018 |pmid=29999197 |pmc=6175393 |doi=10.1111/pde.13612 |display-authors=6 }}

== External links == * {{cite web | url = https://druginfo.nlm.nih.gov/drugportal/name/abametapir | archive-url = https://web.archive.org/web/20201127181917/https://druginfo.nlm.nih.gov/drugportal/name/abametapir | url-status = dead | archive-date = 27 November 2020 | publisher = U.S. National Library of Medicine | work = Drug Information Portal | title = Abametapir }}

Category:Antiparasitic agents Category:Lice

Abametapir

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