WYNZORA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for WYNZORA (WYNZORA).
WYNZORA (halobetasol propionate and tazarotene) is a fixed-dose combination of a corticosteroid (halobetasol) and a retinoid (tazarotene). Halobetasol acts by inducing phospholipase A2 inhibitory proteins, collectively called lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Tazarotene is a retinoid prodrug that is converted to its active metabolite tazarotenic acid, which binds to retinoic acid receptors (RAR-γ, RAR-α, and RAR-β) and modulates gene expression, reducing epidermal proliferation and differentiation.
| Metabolism | Halobetasol is metabolized primarily in the liver via reduction and conjugation; tazarotene is rapidly metabolized by ester hydrolysis to its active metabolite tazarotenic acid, which is further metabolized via oxidation to sulfoxides and sulfones, and then conjugated. Less than 1% of topically applied dose is systemically absorbed. |
| Excretion | Renal: 60% as unchanged drug; Fecal: 30% as metabolites and unchanged drug. |
| Half-life | Terminal elimination half-life: 24 hours; supports once-daily dosing. |
| Protein binding | >99% bound primarily to albumin. |
| Volume of Distribution | Vd: 2 L/kg; indicates extensive tissue distribution. |
| Bioavailability | Topical: <5% systemic absorption; minimizes systemic effects. |
| Onset of Action | Topical: Clinical effect observed within 1-2 weeks. |
| Duration of Action | Topical: Effect persists for 24 hours after single application; continuous use required for sustained benefit. |
| Molecular Weight | 145000 |
Adults: Apply a thin layer to affected areas twice daily (morning and evening) for up to 4 weeks. For scalp application, use once daily. Maximum weekly dose: 100 g.
| Dosage form | CREAM |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established. |
| Geriatric use | No specific dose adjustment recommended; use caution due to potential for increased sensitivity and skin atrophy. |
| 1st trimester | WYNSORA (bimekizumab) is a humanized monoclonal IgG1 antibody. In pregnancy, IgG antibodies are known to cross the placenta, particularly during the third trimester. Limited human data are available for bimekizumab in the first trimester; however, based on its mechanism (IL-17A and IL-17F inhibition), there is potential risk to the developing fetal immune system. Animal studies have not shown direct or indirect harmful effects with respect to reproductive toxicity. Use only if clearly needed. |
| 2nd trimester | During the second trimester, placental transfer of IgG antibodies increases progressively. Bimekizumab may cross the placenta, potentially affecting fetal immune development. No adequate human studies exist. Consider risk-benefit; use is generally avoided unless maternal benefit outweighs potential fetal risk. |
| 3rd trimester | In the third trimester, IgG antibodies are actively transferred across the placenta, resulting in infant serum levels comparable to maternal levels at birth. Bimekizumab may cause immunosuppression in the neonate. Use is generally not recommended during the third trimester unless essential. |
Clinical note
Comprehensive clinical and safety monograph for WYNZORA (WYNZORA).
| Placental transfer |
■ FDA Black Box Warning
None. However, tazarotene is a teratogen; pregnancy must be excluded before use.
| Serious Effects |
Active serious infectionKnown hypersensitivity to bimekizumab or any excipients
| Precautions | Pregnancy: Avoid use due to teratogenicity of tazarotene (Pregnancy Category X), May cause local skin reactions (burning, stinging, pruritus, erythema, peeling, dry skin), Avoid contact with eyes, mouth, and mucous membranes, Not for use on broken or infected skin, Avoid excessive exposure to natural or artificial sunlight during treatment |
| Food/Dietary | No significant food interactions. Salicylic acid absorption can be increased by co-administration with methotrexate or NSAIDs; avoid concurrent use of topical products containing other keratolytic agents. |
Loading safety data…
| Bimekizumab is a humanized IgG1 monoclonal antibody; as such, it is expected to cross the placenta. Placental transfer of IgG increases as pregnancy progresses, with the greatest transfer occurring in the third trimester. Animal studies have not specifically evaluated placental transfer, but human data on IgG antibodies indicate transfer occurs. The degree is likely similar to other IgG1 antibodies (approximately 50-100% maternal serum levels in cord blood at term). |
| Breastfeeding | It is unknown whether bimekizumab is excreted in human milk. Human IgG antibodies are known to be present in breast milk, but typically in low amounts and are digested in the infant's gastrointestinal tract. However, systemic absorption could occur. Due to the potential for adverse reactions in the breastfed infant (e.g., immunosuppression), the developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for WYNSORA and any potential adverse effects on the breastfed child. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | WYNZORA (halobetasol propionate and tazarotene) is contraindicated in pregnancy. Tazarotene is a teratogen. First trimester: highest risk of congenital anomalies including CNS, craniofacial, cardiovascular defects. Second/third trimester: continued risk; avoid exposure. Topical use may have systemic absorption; strict avoidance recommended. |
| Fetal Monitoring | Pregnancy test before initiation; confirm negative status. Monitor for signs of systemic corticosteroid effects (e.g., adrenal suppression) in mother; fetal ultrasound if exposure occurs. Assess for hypervitaminosis A symptoms from tazarotene. |
| Fertility Effects | In animal studies, tazarotene caused reduced fertility at high oral doses. Halobetasol may impair fertility via corticosteroid-mediated effects. Clinical relevance unknown; advise reproductive-aged patients on effective contraception. |
| Clinical Pearls | WYNZORA (clobetasol propionate and salicylic acid) is a fixed-dose combination for plaque psoriasis. Titrate from low to high potency due to clobetasol's super-high potency. Limit use to 2 consecutive weeks and ≤50 g/week to avoid HPA axis suppression. Salicylic acid enhances penetration and keratolytic effect. Avoid use on face, axillae, groin, or in patients with diabetes or impaired renal function. |
| Patient Advice | Apply a thin layer only to psoriasis plaques, not to unaffected skin or mucous membranes. · Use no more than 2 consecutive weeks; do not exceed 50 grams per week or 24 doses per day. · Wash hands after application unless treating hands; avoid covering treated area with bandages unless directed. · Report signs of skin thinning, striae, burning, or irritation; avoid contact with eyes. · Inform your doctor if you are pregnant, breastfeeding, or using other topical medications. |