Delgocitinib

Q: Is Delgocitinib available over the counter?

Delgocitinib is a prescription medication. You will need a valid prescription from a licensed healthcare provider.

Prescription

الأسماء التجارية: Anzupgo

الشكل الصيدلاني

Topical

طريق الإعطاء

TOPICAL

الشركة المصنِّعة

LEO Pharma, Inc

About This Medication

11 DESCRIPTION ANZUPGO (delgocitinib) cream is a white to slightly brown cream for topical use and contains delgocitinib as the active ingredient. Delgocitinib is a white to almost white powder. Delgocitinib is slightly soluble in aqueous solutions at pH 5.0. The pKa of delgocitinib is 5.5. Delgocitinib is a Janus kinase (JAK) inhibitor [JAK1, JAK2, JAK3, and tyrosine kinase 2 (TYK2)] with the chemical name 3-[(3S,4R)-3-Methyl- 6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3- oxopropanenitrile. The molecular formula is C 16 H 18 N 6 O and the molecular weight is 310.35 g/mol. Delgocitinib has the structural formula: Each gram of ANZUPGO contains 20 mg of delgocitinib. Inactive ingredients include benzyl alcohol, butylated hydroxyanisole, cetostearyl alcohol, citric acid monohydrate, edetate disodium, hydrochloric acid, mineral oil, polyoxyl 20 cetostearyl ether, and purified water. Chemical Structure

المواد الفعالة

المادة الفعالة	التركيز
Delgocitinib	-

المؤشرات العلاجية والاستخدام

1 INDICATIONS AND USAGE ANZUPGO is indicated for the topical treatment of moderate to severe chronic hand eczema (CHE) in adults who have had an inadequate response to, or for whom topical corticosteroids are not advisable. ANZUPGO is a Janus kinase (JAK) inhibitor indicated for the topical treatment of moderate to severe chronic hand eczema (CHE) in adults who have had an inadequate response to, or for whom topical corticosteroids are not advisable. ( 1 ) Limitations of Use: Use of ANZUPGO in combination with other JAK inhibitors or potent immunosuppressants is not recommended. ( 1 ) Limitations of Use Use of ANZUPGO in combination with other JAK inhibitors or potent immunosuppressants is not recommended.

آلية العمل

12.1 Mechanism of Action Delgocitinib, a Janus kinase (JAK) inhibitor, inhibits the activity of JAK1, JAK2, JAK3, and tyrosine kinase 2 (TYK2). JAK signaling involves recruitment of signal transducers and activators of transcription (STATs) to cytokine receptors, and activation and subsequent localization of STATs to the nucleus, leading to the expression of cytokine-responsive genes to induce specific biological responses in target cells. The exact mechanism of action of delgocitinib in the treatment of moderate to severe CHE is currently not known.

الجرعة وطريقة الإعطاء

2 DOSAGE AND ADMINISTRATION See the full prescribing information for recommended immunizations prior to treatment. ( 2.1 ) Do not use more than 30 grams per 2 weeks or 60 grams per month. Apply twice daily to skin of the affected areas only on the hands and wrists. ( 2.2 ) For topical use only. Not for oral, ophthalmic, or intravaginal use. ( 2.2 ) 2.1 Recommended Immunizations Prior to Treatment Initiation Complete any necessary immunizations, including herpes zoster vaccinations, according to current immunization guidelines prior to ANZUPGO treatment [see Warnings and Precautions (5.3) ]. 2.2 Recommended Dosage and Administration Do not use more than 30 grams per 2 weeks or 60 grams per month. Prior to applying ANZUPGO, clean and dry affected areas. Apply a thin layer of ANZUPGO, twice daily, to the affected areas only on the hands and wrists. ANZUPGO is for topical use only. Not for oral, ophthalmic, or intravaginal use. Avoid contact with eyes, mouth, or other mucous membranes. If contact with mucous membranes occurs, rinse thoroughly with water.

Side Effects Overview

6 ADVERSE REACTIONS Adverse reactions that were reported in ≤ 1% of subjects were application site pain, paresthesia, pruritus, erythema, and bacterial skin infections including finger cellulitis, paronychia, other skin infections, leukopenia, and neutropenia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact LEO Pharma Inc. at 1-877-494-4536 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The safety of ANZUPGO was evaluated in two randomized, double-blind, multicenter, vehicle-controlled clinical trials (TRIAL 1 and TRIAL 2), in which 959 adults with moderate to severe CHE received ANZUPGO or vehicle cream topically twice daily for 16 weeks. A total of 638 subjects were treated with ANZUPGO [see Clinical Studies (14) ] . In TRIAL 1 and TRIAL 2, adverse reactions that were reported in ≤ 1% of subjects in the ANZUPGO group were application site pain, paresthesia, pruritus, erythema, and bacterial skin infections including finger cellulitis, paronychia, other skin infections, leukopenia, and neutropenia. In an open label extension trial (TRIAL 3), 801 subjects were treated for up to an additional 36 weeks after completing TRIAL 1 or TRIAL 2. A total of 198 subjects received continuous treatment with ANZUPGO for 52 weeks. Eczema herpeticum was observed in one subject and herpes zoster was observed in two subjects treated with ANZUPGO.

التحذيرات والاحتياطات

5 WARNINGS AND PRECAUTIONS Serious Infections: ANZUPGO may increase the risk of infection. Eczema herpeticum was observed in a subject treated topically with ANZUPGO. Avoid use of ANZUPGO in patients with an active or serious infection. If a serious infection develops, discontinue ANZUPGO until the infection resolves. ( 5.1 ) Non-melanoma Skin Cancers: Non-melanoma skin cancers including basal cell carcinoma have been reported in subjects treated with ANZUPGO. Periodic skin examinations are recommended for all patients, particularly those with risk factors for skin cancer. ( 5.2 ) Immunizations: Avoid vaccination with live vaccines immediately prior to, during, and immediately after ANZUPGO treatment. ( 5.3 ) Potential Risks Related to JAK Inhibition: It is not known whether ANZUPGO may be associated with the observed or potential adverse reactions of JAK inhibition. Higher rates of all-cause mortality, including sudden cardiovascular death, major adverse cardiovascular events, overall thrombosis, deep venous thrombosis, pulmonary embolism, and malignancies (excluding non-melanoma skin cancer) were observed in patients treated with a JAK inhibitor compared to those treated with TNF blockers in rheumatoid arthritis (RA) patients. ANZUPGO is not approved for use in RA. Treatment with oral and topical JAK inhibitors has been associated with increases in lipid parameters including total cholesterol, low-density lipoprotein (LDL) cholesterol, and triglycerides. ( 5.4 ) 5.1 Serious Infections ANZUPGO may increase the risk of infections. Eczema herpeticum was observed in a subject treated with ANZUPGO [see Adverse Reactions (6.1) ]. Serious and sometimes fatal infections due to bacterial, mycobacterial, invasive fungal, viral, or other opportunistic pathogens have been reported in patients receiving oral or topical JAK inhibitors [see Adverse Reactions (6.1) ]. Avoid use of ANZUPGO in patients with an active or serious infection. Consider the risks and benefits of treatment prior to initiating ANZUPGO in patients: with chronic or recurrent infection who have been exposed to tuberculosis with a history of a serious or an opportunistic infection with underlying conditions that may predispose them to infection. Closely monitor patients for the development of signs and symptoms of infection during and after treatment with ANZUPGO. A patient who develops a new infection during treatment with ANZUPGO should undergo prompt and complete diagnostic testing; appropriate antimicrobial therapy should be initiated; and the patient should be closely monitored. Interrupt treatment with ANZUPGO if a patient develops a serious infection. Do not resume ANZUPGO until the infection resolves or is adequately treated. Viral Reactivation Viral reactivation, including cases of herpes virus reactivation (e.g., herpes zoster), were reported in clinical trials with ANZUPGO. If a patient develops herpes zoster, consider interrupting ANZUPGO treatment until the episode resolves. The impact of ANZUPGO on chronic viral hepatitis reactivation is unknown. Patients with active hepatitis B or C infection were excluded from clinical trials with ANZUPGO. Consider viral hepatitis screening and monitoring for reactivation in accordance with clinical guidelines before starting therapy and during therapy with ANZUPGO. If signs of reactivation occur, consult a hepatitis specialist. ANZUPGO is not recommended for use in patients with active hepatitis B or hepatitis C. 5.2 Non-melanoma Skin Cancers Non-melanoma skin cancers including basal cell carcinoma have been reported in subjects treated with ANZUPGO. Periodic skin examinations of the application sites are recommended for all patients, particularly those with risk factors for skin cancer. Advise patients to avoid sunlamps and minimize exposure to sunlight by wearing sun-protective clothing or using broad-spectrum sunscreen. 5.3 Immunizations Prior to ANZUPGO treatment, complete all age-appropriate vaccinations as recommended by current immunization guidelines, including herpes zoster vaccinations. Avoid vaccination with live vaccines immediately prior to, during, and immediately after ANZUPGO treatment. 5.4 Potential Risks Related to JAK Inhibition It is not known whether ANZUPGO may be associated with the observed or potential adverse reactions of JAK inhibition. In a large, randomized, postmarketing safety trial of an oral JAK inhibitor in combination with methotrexate in rheumatoid arthritis (RA), patients 50 years of age and older with at least one cardiovascular risk factor, higher rates of all-cause mortality, including sudden cardiovascular death, major adverse cardiovascular events (MACE), overall thrombosis, deep venous thrombosis (DVT), pulmonary embolism (PE), and malignancies (excluding non-melanoma skin cancer) were observed in patients treated with the JAK inhibitor compared to those treated with TNF blockers. ANZUPGO is not indicated for use in RA. Treatment with oral and topical JAK inhibitors has been associated with increases in lipid parameters including total cholesterol, low-density lipoprotein (LDL) cholesterol, and triglycerides.

موانع الاستعمال

4 CONTRAINDICATIONS None None. ( 4 )

الحرائك الدوائية

12.3 Pharmacokinetics The pharmacokinetics of ANZUPGO were evaluated in a pharmacokinetic (PK) trial involving 15 adult subjects 22 to 69 years of age with moderate to severe CHE and in 313 subjects in TRIAL 2 [see Clinical Studies (14) ]. Absorption In the PK trial, subjects applied on average 0.87 g of ANZUPGO topically to the affected areas of the hands and wrists twice a day for 8 days. The mean ± SD maximum plasma concentration (C max ) and area under the concentration-curve from time 0 to 12 hours (AUC 0-12 ) on Day 1 was 1.53 ng/mL ± 2.24 and 6.1 ng*h/mL ± 8.14, respectively. The lower limit of quantification was 0.005 ng/mL in the assay. The systemic exposure (AUC and Cmax) between Day 1 and Day 8 were similar. There was no evidence of accumulation with twice daily topical application of ANZUPGO. In TRIAL 2, a single PK sample was assessed between 2-6 hours following twice daily application of ANZUPGO. The mean plasma concentration on Weeks 1, 4, and 16 were 0.42 ng/mL, 0.50 ng/mL, and 0.35 ng/mL, respectively. Distribution Plasma protein binding of delgocitinib is 22 to 29%. Elimination Following repeated topical application of ANZUPGO, the average half-life of delgocitinib was estimated to be 21 hours. Metabolism Delgocitinib does not undergo extensive metabolism and the main plasma component is unchanged delgocitinib. Following oral administration, four metabolites (formed via oxidation and glucuronide conjugation) were detected at < 2% of the average unchanged delgocitinib plasma concentrations. The limited metabolism of delgocitinib occurs primarily though CYP3A4/5 and to a lesser extent by CYP1A1, CYP2C9, CYP2C19, and CYP2D6. Excretion Delgocitinib is primarily eliminated by renal excretion as approximately 75% of the total dose after oral administration was found unchanged in the urine. Drug Interaction Studies Clinical Studies Drug interaction studies with ANZUPGO have not been conducted. In Vitro Studies Delgocitinib does not inhibit or induce cytochrome P450 enzymes or inhibit transporter systems such as P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), organic anion transporting proteins (OATP), organic anion transporters (OAT), organic cation transporters (OCT), or multidrug and toxin extrusion protein (MATE) at clinically relevant concentrations.

Frequently Asked Questions

1 INDICATIONS AND USAGE ANZUPGO is indicated for the topical treatment of moderate to severe chronic hand eczema (CHE) in adults who have had an inadequate response to, or for whom topical corticosteroids are not advisable. ANZUPGO is a Janus kinase (JAK) inhibitor indicated for the topical treatment of moderate to severe chronic hand eczema (CHE) in adults who have had an inadequate response to, or for whom topical corticosteroids are not advisable. ( 1 ) Limitations of Use: Use …

2 DOSAGE AND ADMINISTRATION See the full prescribing information for recommended immunizations prior to treatment. ( 2.1 ) Do not use more than 30 grams per 2 weeks or 60 grams per month. Apply twice daily to skin of the affected areas only on the hands and wrists. ( 2.2 ) For topical use only. Not for oral, ophthalmic, or intravaginal use. ( 2.2 ) 2.1 Recommended Immunizations Prior to Treatment Initiation Complete any necessary immunizations, including herpes zoster vaccinations, …

5 WARNINGS AND PRECAUTIONS Serious Infections: ANZUPGO may increase the risk of infection. Eczema herpeticum was observed in a subject treated topically with ANZUPGO. Avoid use of ANZUPGO in patients with an active or serious infection. If a serious infection develops, discontinue ANZUPGO until the infection resolves. ( 5.1 ) Non-melanoma Skin Cancers: Non-melanoma skin cancers including basal cell carcinoma have been reported in subjects treated with ANZUPGO. Periodic skin examinations are recommended for all patients, particularly those with risk …

4 CONTRAINDICATIONS None None. ( 4 )

Delgocitinib is a prescription medication. You will need a valid prescription from a licensed healthcare provider.

References & Data Sources

• DailyMed — Delgocitinib drug label (National Library of Medicine)
• openFDA — Delgocitinib label data (U.S. Food & Drug Administration)
• RxNorm — RXCUI 2721167 (NLM Normalized Drug Names)
• NDC Directory — Delgocitinib (FDA National Drug Code)

إخلاء المسؤولية الطبية

المعلومات الواردة في هذه الصفحة مخصصة للأغراض التعليمية فقط ولا ينبغي استخدامها بديلًا عن المشورة الطبية المتخصصة أو التشخيص أو العلاج.

استشر دائمًا طبيبك أو أي مقدم رعاية صحية مؤهل بشأن أي أسئلة تتعلق بحالة طبية أو دواء.

مصادر البيانات: DailyMed (NLM), openFDA, MFDS