Abametapir

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.[1][2]

Abametapir
Clinical data
Trade namesXeglyze
Other namesHa44
AHFS/Drugs.comProfessional Drug Facts
License data
Routes of
administration		Topical
Drug classPediculicide, metalloproteinase inhibitor
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding91.3–92.3%
MetabolismCYP1A2
MetabolitesHydroxyl and carboxyl derivatives
Elimination half-life21 hours
Identifiers
IUPAC name
  • 5,5'-dimethyl-2,2'-bipyridine
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.157.434
Chemical and physical data
FormulaC12H12N2
Molar mass184.242 g·mol−1
3D model (JSmol)
SMILES
  • CC1=CN=C(C=C1)C2=NC=C(C=C2)C
InChI
  • InChI=1S/C12H12N2/c1-9-3-5-11(13-7-9)12-6-4-10(2)8-14-12/h3-8H,1-2H3
  • Key:PTRATZCAGVBFIQ-UHFFFAOYSA-N

The most common side effects include skin redness, rash, skin burning sensation, skin inflammation, vomiting, eye irritation, skin itching, and hair color changes.[2]

Abametapir is a metalloproteinase inhibitor.[1] Abametapir was approved for medical use in the United States in July 2020.[1][3] The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[4]

Medical uses

Abametapir is indicated for the topical treatment of head lice infestation in people six months of age and older.[1][2]

Contraindications

Abametapir has no contraindications according to the labeling.[5]

Adverse effects

Common adverse effects are burning skin sensations (in 3% of patients), contact dermatitis (2%), skin redness (4%), rash (3%), and vomiting (2%).[5]

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.[1]

Pharmacology

Mechanism of action

The drug inhibits enzymes called metalloproteinases. In lice, these enzymes play a role in egg development and survival;[1] 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 Cmax 30 times and an area under the curve (AUC) 250 times that of abametapir itself.[1]

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.[1]

The drug's metabolites in humans: abametapir hydroxyl (left) and abametapir carboxyl (right)[1]

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.[2] The trials were conducted at fourteen sites in the United States.[2]

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.[2]

About half of all enrolled participants was randomly assigned to abametapir and the other half to placebo.[2] Abametapir lotion or placebo lotion were applied once as a ten-minute treatment to infested hair.[2] 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.[2]

References
  1. "Xeglyze (abametapir) lotion, for topical use" (PDF). U.S. Food and Drug Administration (FDA). Dr. Reddy's Laboratories. Inc. Retrieved 25 July 2020.
  2. "Drug Trial Snapshot: Xeglyze". U.S. Food and Drug Administration (FDA). 24 July 2020. Retrieved 6 August 2020. This article incorporates text from this source, which is in the public domain.
  3. "Drug Approval Package: Xeglyze". U.S. Food and Drug Administration (FDA). 21 August 2020. Retrieved 17 January 2021.
  4. "New Drug Therapy Approvals 2020". U.S. Food and Drug Administration (FDA). 31 December 2020. Retrieved 17 January 2021. This article incorporates text from this source, which is in the public domain.
  5. Abametapir Professional Drug Facts. Accessed 6 May 2021.

Further reading
  • "Abametapir". Drug Information Portal. U.S. National Library of Medicine.
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