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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]
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| Clinical data | |
|---|---|
| Trade names | Xeglyze |
| Other names | Ha44 |
| AHFS/Drugs.com | Professional Drug Facts |
| License data |
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| Routes of administration | Topical |
| Drug class | Pediculicide, metalloproteinase inhibitor |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Protein binding | 91.3–92.3% |
| Metabolism | CYP1A2 |
| Metabolites | Hydroxyl and carboxyl derivatives |
| Elimination half-life | 21 hours |
| Identifiers | |
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| CAS Number | |
| PubChem CID | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEMBL | |
| PDB ligand | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.157.434 |
| Chemical and physical data | |
| Formula | C12H12N2 |
| Molar mass | 184.242 g·mol−1 |
| 3D model (JSmol) | |
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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]
Abametapir is indicated for the topical treatment of head lice infestation in people six months of age and older.[1][2]
Abametapir has no contraindications according to the labeling.[5]
Common adverse effects are burning skin sensations (in 3% of patients), contact dermatitis (2%), skin redness (4%), rash (3%), and vomiting (2%).[5]
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]
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 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]
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