Peringatan Keamanan

Patients experiencing an acute overdose may present with fluid retention and hypoglycemia followed by hyperglycemia.^L36380 Chronic overdosage may present with signs of gigantism.^L36380 Treat patients with symptomatic and supportive measures.

Lonapegsomatropin

DB16220

biotech approved investigational

Deskripsi

Lonapegsomatropin, also known as TransCon hGH or ACP 001, is a methoxypegylated prodrug of human growth hormone (somatropin) indicated for the treatment of children 1 year and older, weighing at least 11.5 kg, with growth failure due to insufficient growth hormone secretion.A237605,L36380,L36405 Unlike somatropin, which requires daily dosing, lonapegsomatropin can be administered as a single weekly dose.L36380,L10971

Lonapegsomatropin was granted FDA approval on 25 August 2021.^L36380 It was later approved by the European Commission on 13 January 2022.^L39900

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of lonapegsomatropin-tcgd is 30.7 ± 12.7 hours, while the half life of released [somatropin] was approximately 25 hours.[L36380]

Volume Distribusi Lonapegsomatropin-tcgd dosing of 0.24 mg/kg/week leads to a mean steady state apparent volume of distribution of 0.13 L/kg.[L36380]

Klirens (Clearance) In pediatric patients, the apparent clearance of lonapegsomatropin-tcgd is 3.2 mL/h/kg.[L36380]

Absorpsi

After subcutaneous lonapegsomatropin-tcgd administration, the drug undergoes autocleavage, releasing active somatropin from the methoxypolyethylene glycol carrier.^L36380 0.24 mg/kg/week dosing in pediatric patients leads to a somatropin C_max of 15.2 ng/mL, with a median T_max of 12 hours, and a mean AUC of 500 h\*ng/mL.^L36380 Methoxypolyethylene glycol reaches a C_max of 13.1 µg/mL, with a meadian T_max of 36 hours.^L36380 Human growth hormone (somatropin) concentrations reach a mean steady C_max of 1230 ng/mL, with a T_max of 25 hours.^L36380

Metabolisme

Lonapegsomatropin-tcgd is a prodrug that undergoes autocleavage, releasing the active somatropin from the methoxypolyethelene glycol carrier.^L36380 The methoxypolyethelene glycol carrier is cleared by the kidneys, while somatropin is metabolized by non-specific protein catabolic pathways in the liver and kidneys to smaller oligopeptides and individual amino acids.^L36380

Rute Eliminasi

The methoxypolyethelene glycol carrier is cleared by the kidneys, while the active somatropin undergoes catabolic processes in the kidneys and liver.^L36380 However, the exact proportions of lonapegsomatropin recovered in the urine and feces has not been reported.

Interaksi Obat

335 Data

Medrysone	The serum concentration of the active metabolites of Medrysone can be decreased when Medrysone is used in combination with Lonapegsomatropin.
Amcinonide	The serum concentration of the active metabolites of Amcinonide can be decreased when Amcinonide is used in combination with Lonapegsomatropin.
Fluorometholone	The serum concentration of the active metabolites of Fluorometholone can be decreased when Fluorometholone is used in combination with Lonapegsomatropin.
Beclomethasone dipropionate	The serum concentration of the active metabolites of Beclomethasone dipropionate can be decreased when Beclomethasone dipropionate is used in combination with Lonapegsomatropin.
Betamethasone	The serum concentration of the active metabolites of Betamethasone can be decreased when Betamethasone is used in combination with Lonapegsomatropin.
Triamcinolone	The serum concentration of the active metabolites of Triamcinolone can be decreased when Triamcinolone is used in combination with Lonapegsomatropin.
Prednisone	The serum concentration of the active metabolites of Prednisone can be decreased when Prednisone is used in combination with Lonapegsomatropin.
Mometasone	The serum concentration of the active metabolites of Mometasone can be decreased when Mometasone is used in combination with Lonapegsomatropin.
Rimexolone	The serum concentration of the active metabolites of Rimexolone can be decreased when Rimexolone is used in combination with Lonapegsomatropin.
Clobetasol propionate	The serum concentration of the active metabolites of Clobetasol propionate can be decreased when Clobetasol propionate is used in combination with Lonapegsomatropin.
Fluocinonide	The serum concentration of the active metabolites of Fluocinonide can be decreased when Fluocinonide is used in combination with Lonapegsomatropin.
Cortisone acetate	The serum concentration of the active metabolites of Cortisone acetate can be reduced when Cortisone acetate is used in combination with Lonapegsomatropin resulting in a loss in efficacy.
Paramethasone	The serum concentration of the active metabolites of Paramethasone can be decreased when Paramethasone is used in combination with Lonapegsomatropin.
Ciclesonide	The serum concentration of the active metabolites of Ciclesonide can be decreased when Ciclesonide is used in combination with Lonapegsomatropin.
Fluticasone furoate	The serum concentration of the active metabolites of Fluticasone furoate can be decreased when Fluticasone furoate is used in combination with Lonapegsomatropin.
Fluprednidene	The serum concentration of the active metabolites of Fluprednidene can be decreased when Fluprednidene is used in combination with Lonapegsomatropin.
Fluocortolone	The serum concentration of the active metabolites of Fluocortolone can be decreased when Fluocortolone is used in combination with Lonapegsomatropin.
Difluocortolone	The serum concentration of the active metabolites of Difluocortolone can be decreased when Difluocortolone is used in combination with Lonapegsomatropin.
Meprednisone	The serum concentration of the active metabolites of Meprednisone can be decreased when Meprednisone is used in combination with Lonapegsomatropin.
Dexamethasone isonicotinate	The serum concentration of the active metabolites of Dexamethasone isonicotinate can be decreased when Dexamethasone isonicotinate is used in combination with Lonapegsomatropin.
Clobetasol	The serum concentration of the active metabolites of Clobetasol can be decreased when Clobetasol is used in combination with Lonapegsomatropin.
Deflazacort	The serum concentration of the active metabolites of Deflazacort can be decreased when Deflazacort is used in combination with Lonapegsomatropin.
Cortivazol	The serum concentration of the active metabolites of Cortivazol can be decreased when Cortivazol is used in combination with Lonapegsomatropin.
Prednylidene	The serum concentration of the active metabolites of Prednylidene can be decreased when Prednylidene is used in combination with Lonapegsomatropin.
Halometasone	The serum concentration of the active metabolites of Halometasone can be decreased when Halometasone is used in combination with Lonapegsomatropin.
Cloprednol	The serum concentration of the active metabolites of Cloprednol can be decreased when Cloprednol is used in combination with Lonapegsomatropin.
Fluticasone	The serum concentration of the active metabolites of Fluticasone can be decreased when Fluticasone is used in combination with Lonapegsomatropin.
Mometasone furoate	The serum concentration of the active metabolites of Mometasone furoate can be decreased when Mometasone furoate is used in combination with Lonapegsomatropin.
Prednisolone phosphate	The serum concentration of the active metabolites of Prednisolone phosphate can be decreased when Prednisolone phosphate is used in combination with Lonapegsomatropin.
Prednisolone hemisuccinate	The serum concentration of the active metabolites of Prednisolone hemisuccinate can be decreased when Prednisolone hemisuccinate is used in combination with Lonapegsomatropin.
Fluprednidene acetate	The serum concentration of the active metabolites of Fluprednidene acetate can be decreased when Fluprednidene acetate is used in combination with Lonapegsomatropin.
Methylprednisolone hemisuccinate	The serum concentration of the active metabolites of Methylprednisolone hemisuccinate can be decreased when Methylprednisolone hemisuccinate is used in combination with Lonapegsomatropin.
Prednisone acetate	The serum concentration of the active metabolites of Prednisone acetate can be decreased when Prednisone acetate is used in combination with Lonapegsomatropin.
Clocortolone acetate	The serum concentration of the active metabolites of Clocortolone acetate can be decreased when Clocortolone acetate is used in combination with Lonapegsomatropin.
Melengestrol acetate	The serum concentration of the active metabolites of Melengestrol acetate can be decreased when Melengestrol acetate is used in combination with Lonapegsomatropin.
Betamethasone phosphate	The serum concentration of the active metabolites of Betamethasone phosphate can be decreased when Betamethasone phosphate is used in combination with Lonapegsomatropin.
Cortisone	The serum concentration of the active metabolites of Cortisone can be decreased when Cortisone is used in combination with Lonapegsomatropin.
Diethylstilbestrol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Diethylstilbestrol.
Chlorotrianisene	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Chlorotrianisene.
Conjugated estrogens	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Conjugated estrogens.
Estradiol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Estradiol.
Ethinylestradiol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Ethinylestradiol.
Mestranol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Mestranol.
Estriol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Estriol.
Estrone sulfate	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Estrone sulfate.
Quinestrol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Quinestrol.
Hexestrol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Hexestrol.
Tibolone	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Tibolone.
Synthetic Conjugated Estrogens, A	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Synthetic Conjugated Estrogens, A.
Synthetic Conjugated Estrogens, B	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Synthetic Conjugated Estrogens, B.
Polyestradiol phosphate	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Polyestradiol phosphate.
Esterified estrogens	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Esterified estrogens.
Zeranol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Zeranol.
Equol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Equol.
Estetrol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Estetrol.
Methallenestril	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Methallenestril.
Epimestrol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Epimestrol.
Moxestrol	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Moxestrol.
Estradiol acetate	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Estradiol acetate.
Estradiol valerate	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Estradiol valerate.
Biochanin A	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Biochanin A.
Formononetin	The therapeutic efficacy of Lonapegsomatropin can be decreased when used in combination with Formononetin.
Insulin human	The therapeutic efficacy of Insulin human can be decreased when used in combination with Lonapegsomatropin.
Insulin lispro	The therapeutic efficacy of Insulin lispro can be decreased when used in combination with Lonapegsomatropin.
Insulin glargine	The therapeutic efficacy of Insulin glargine can be decreased when used in combination with Lonapegsomatropin.
Insulin pork	The therapeutic efficacy of Insulin pork can be decreased when used in combination with Lonapegsomatropin.
Troglitazone	The therapeutic efficacy of Troglitazone can be decreased when used in combination with Lonapegsomatropin.
Glimepiride	The therapeutic efficacy of Glimepiride can be decreased when used in combination with Lonapegsomatropin.
Sulfisoxazole	The therapeutic efficacy of Sulfisoxazole can be decreased when used in combination with Lonapegsomatropin.
Disopyramide	The therapeutic efficacy of Disopyramide can be decreased when used in combination with Lonapegsomatropin.
Acarbose	The therapeutic efficacy of Acarbose can be decreased when used in combination with Lonapegsomatropin.
Metformin	The therapeutic efficacy of Metformin can be decreased when used in combination with Lonapegsomatropin.
Sulfadiazine	The therapeutic efficacy of Sulfadiazine can be decreased when used in combination with Lonapegsomatropin.
Rosiglitazone	The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Lonapegsomatropin.
Acetohexamide	The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Lonapegsomatropin.
Quinine	The therapeutic efficacy of Quinine can be decreased when used in combination with Lonapegsomatropin.
Miglitol	The therapeutic efficacy of Miglitol can be decreased when used in combination with Lonapegsomatropin.
Chlorpropamide	The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Lonapegsomatropin.
Nateglinide	The therapeutic efficacy of Nateglinide can be decreased when used in combination with Lonapegsomatropin.
Pentamidine	The therapeutic efficacy of Pentamidine can be decreased when used in combination with Lonapegsomatropin.
Mifepristone	The therapeutic efficacy of Mifepristone can be decreased when used in combination with Lonapegsomatropin.
Tolazamide	The therapeutic efficacy of Tolazamide can be decreased when used in combination with Lonapegsomatropin.
Repaglinide	The therapeutic efficacy of Repaglinide can be decreased when used in combination with Lonapegsomatropin.
Phenformin	The therapeutic efficacy of Phenformin can be decreased when used in combination with Lonapegsomatropin.
Sulfamethoxazole	The therapeutic efficacy of Sulfamethoxazole can be decreased when used in combination with Lonapegsomatropin.
Glyburide	The therapeutic efficacy of Glyburide can be decreased when used in combination with Lonapegsomatropin.
Glipizide	The therapeutic efficacy of Glipizide can be decreased when used in combination with Lonapegsomatropin.
Gliclazide	The therapeutic efficacy of Gliclazide can be decreased when used in combination with Lonapegsomatropin.
Tolbutamide	The therapeutic efficacy of Tolbutamide can be decreased when used in combination with Lonapegsomatropin.
Pioglitazone	The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Lonapegsomatropin.
Bromocriptine	The therapeutic efficacy of Bromocriptine can be decreased when used in combination with Lonapegsomatropin.
Gliquidone	The therapeutic efficacy of Gliquidone can be decreased when used in combination with Lonapegsomatropin.
Mitiglinide	The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Lonapegsomatropin.
Sitagliptin	The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Lonapegsomatropin.
Sunitinib	The therapeutic efficacy of Sunitinib can be decreased when used in combination with Lonapegsomatropin.
Exenatide	The therapeutic efficacy of Exenatide can be decreased when used in combination with Lonapegsomatropin.
Mecasermin	The therapeutic efficacy of Mecasermin can be decreased when used in combination with Lonapegsomatropin.
Pramlintide	The therapeutic efficacy of Pramlintide can be decreased when used in combination with Lonapegsomatropin.
Glisoxepide	The therapeutic efficacy of Glisoxepide can be decreased when used in combination with Lonapegsomatropin.
Insulin aspart	The therapeutic efficacy of Insulin aspart can be decreased when used in combination with Lonapegsomatropin.

Target Protein

Growth hormone receptor GHR

Prolactin receptor PRLR

Referensi & Sumber

Artikel (PubMed)

PMID: 34272849
Thornton PS, Maniatis AK, Aghajanova E, Chertok E, Vlachopapadopoulou E, Lin Z, Song W, Christoffersen ED, Breinholt VM, Kovalenko T, Giorgadze E, Korpal-Szczyrska M, Hofman PL, Karpf DB, Shu AD, Beckert M: Weekly Lonapegsomatropin in Treatment-Naive Children with Growth Hormone Deficiency: The Phase 3 heiGHt Trial. J Clin Endocrinol Metab. 2021 Jul 17. pii: 6323258. doi: 10.1210/clinem/dgab529.
PMID: 22291494
Reh CS, Geffner ME: Somatotropin in the treatment of growth hormone deficiency and Turner syndrome in pediatric patients: a review. Clin Pharmacol. 2010;2:111-22. doi: 10.2147/CPAA.S6525. Epub 2010 Jun 1.

Link

Contoh Produk & Brand

Produk: 18 • International brands: 1

Produk

Lonapegsomatropin Ascendis Pharma

Injection, powder, for solution • 3 mg • Subcutaneous • EU • Approved
Lonapegsomatropin Ascendis Pharma

Injection, powder, for solution • 3.6 mg • Subcutaneous • EU • Approved
Lonapegsomatropin Ascendis Pharma

Injection, powder, for solution • 4.3 mg • Subcutaneous • EU • Approved
Lonapegsomatropin Ascendis Pharma

Injection, powder, for solution • 5.2 mg • Subcutaneous • EU • Approved
Lonapegsomatropin Ascendis Pharma

Injection, powder, for solution • 6.3 mg • Subcutaneous • EU • Approved
Lonapegsomatropin Ascendis Pharma

Injection, powder, for solution • 7.6 mg • Subcutaneous • EU • Approved
Lonapegsomatropin Ascendis Pharma

Injection, powder, for solution • 9.1 mg • Subcutaneous • EU • Approved
Lonapegsomatropin Ascendis Pharma

Injection, powder, for solution • 11 mg • Subcutaneous • EU • Approved

Menampilkan 8 dari 18 produk.

International Brands

Skytrofa — Ascendis Pharma A/S

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.