Peringatan Keamanan

LD50 information for ferric derisomaltose is not readily available in the literature, however, the LD50 for iron sucrose (another form of intravenous iron) was 140 mg/kg in male rats.^L11635 An overdose with ferric derisomaltose may lead to accumulation of stored iron, causing hemosiderosis.^L11620 Symptoms may include abdominal pain, weakness, and lethargy, among others.^A190588 Serum ferritin should be monitored. Employ supportive treatment including chelating agents.L11581,L11620

Ferric derisomaltose

DB15617

small molecule approved

Deskripsi

Iron deficiency is an extremely common condition and is the most frequent cause of anemia worldwide. Iron deficiency results when iron intake, iron stores, and loss of iron from the body do not adequately support production of erythrocytes, also known as red blood cells. Though it is generally considered non life-threatening, iron deficiency may considerably affect quality of life.^A190528

Ferric derisomaltose is a form of iron used in the treatment of iron deficiency. This drug is a complex of iron (III) hydroxide and derisomaltose. The latter is an iron carbohydrate oligosaccharide that works to release iron. Ferric derisomaltose was developed by Pharmacosmos Therapeutics ad was granted FDA approval in January 2020.L11581,L11587 Clinical trials show that it is non-inferior to iron sucrose, another form of iron that is often administered in iron deficiency, and less likely to cause serious hypersensitivity that is associated with other forms of injectable iron.A190519,A188021

Struktur Molekul 2D

Berat 562.297

Wujud solid

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 plasma-half live of intravenous iron is about 1-4 days.[L11617]

Volume Distribusi Ferric derisomaltose or released iron that was released is found in cells of the reticuloendothelial system (RES). It is found to be highly concentrated in the liver and spleen.[L11617] The volume of distribution of other forms of intravenous iron is 3L, on average, in a 70 kg adult.[A32524] Though the specific volume of distribution of ferric derisomaltose is not readily available in the literature, it is likely similar to other intravenous forms of iron.[A32524]

Klirens (Clearance) Intravenous iron is cleared from the plasma.[A190582] Ferric derisomaltose is not eliminated via the kidneys, as the size of the complex is large and cannot be excreted via the nephron.[L11617]

Absorpsi

After a single 1000 mg dose, the Cmax and AUC of serum iron were 408 ?g/mL and 17730 ?g.h /mL, respectively. Serum ferritin concentrations reach their peak about 7 days after a single dose of intravenous ferric derisomaltose.^L11581 A note on concomitant oral iron The absorption of oral iron is decreased when administered with intravenous iron. The administration of oral iron should be delayed until at least 5 days after the last ferric derisomaltose injection.^L11617

Metabolisme

Iron in the circulation is taken up by the plasma by cells of the RES. This binds proteins that form hemosiderin or ferritin, as well transferrin. Following this step, the bound iron replenishes low hemoglobin (Hb) and iron.^L11617

Rute Eliminasi

Renal elimination was not a significant route of elimination in single-dose pharmacokinetic studies. Iron can often accumulate in the body leading to iron overload followed by toxic effects.^A190582 Small amounts of ferric derisomaltose are excreted in the urine and feces.^L11617

Interaksi Obat

23 Data

Iron Dextran	The absorption of Iron Dextran can be decreased when combined with Ferric derisomaltose.
Iron	The absorption of Iron can be decreased when combined with Ferric derisomaltose.
Prussian blue	The absorption of Prussian blue can be decreased when combined with Ferric derisomaltose.
Iron sucrose	The absorption of Iron sucrose can be decreased when combined with Ferric derisomaltose.
Ferric pyrophosphate	The absorption of Ferric pyrophosphate can be decreased when combined with Ferric derisomaltose.
Ferric ammonium citrate	The absorption of Ferric ammonium citrate can be decreased when combined with Ferric derisomaltose.
Ferumoxsil	The absorption of Ferumoxsil can be decreased when combined with Ferric derisomaltose.
Ferumoxides	The absorption of Ferumoxides can be decreased when combined with Ferric derisomaltose.
Ferric sulfate	The absorption of Ferric sulfate can be decreased when combined with Ferric derisomaltose.
Ferrous bisglycinate	The absorption of Ferrous bisglycinate can be decreased when combined with Ferric derisomaltose.
Gleptoferron	The absorption of Gleptoferron can be decreased when combined with Ferric derisomaltose.
Perflubutane	The absorption of Perflubutane can be decreased when combined with Ferric derisomaltose.
Ferrous sulfate anhydrous	The absorption of Ferrous sulfate anhydrous can be decreased when combined with Ferric derisomaltose.
Sodium feredetate	The absorption of Sodium feredetate can be decreased when combined with Ferric derisomaltose.
Ferric hydroxide	The absorption of Ferric hydroxide can be decreased when combined with Ferric derisomaltose.
Ferric cation	The absorption of Ferric cation can be decreased when combined with Ferric derisomaltose.
Ferrous gluconate	The absorption of Ferrous gluconate can be decreased when combined with Ferric derisomaltose.
Ferrous succinate	The absorption of Ferrous succinate can be decreased when combined with Ferric derisomaltose.
Ferrous fumarate	The absorption of Ferrous fumarate can be decreased when combined with Ferric derisomaltose.
Tetraferric tricitrate decahydrate	The absorption of Tetraferric tricitrate decahydrate can be decreased when combined with Ferric derisomaltose.
Ferric oxyhydroxide	The absorption of Ferric oxyhydroxide can be decreased when combined with Ferric derisomaltose.
Ferric maltol	The absorption of Ferric maltol can be decreased when combined with Ferric derisomaltose.
Iron polymaltose	The absorption of Iron polymaltose can be decreased when combined with Ferric derisomaltose.

Target Protein

Hemoglobin subunit alpha HBA1

Transferrin receptor TFRC

Referensi & Sumber

Synthesis reference: Christensen TS, Andreasen HB.(2019).WO2019048674A1. Retrieved from: https://patents.google.com/patent/WO2019048674A1/en

Artikel (PubMed)

PMID: 31928094
Pollock RF, Biggar P: Indirect methods of comparison of the safety of ferric derisomaltose, iron sucrose and ferric carboxymaltose in the treatment of iron deficiency anemia. Expert Rev Hematol. 2020 Feb;13(2):187-195. doi: 10.1080/17474086.2020.1709437. Epub 2020 Jan 11.
PMID: 31243803
Auerbach M, Henry D, Derman RJ, Achebe MM, Thomsen LL, Glaspy J: A prospective, multi-center, randomized comparison of iron isomaltoside 1000 versus iron sucrose in patients with iron deficiency anemia; the FERWON-IDA trial. Am J Hematol. 2019 Jun 26. doi: 10.1002/ajh.25564.
PMID: 23613366
Miller JL: Iron deficiency anemia: a common and curable disease. Cold Spring Harb Perspect Med. 2013 Jul 1;3(7). pii: cshperspect.a011866. doi: 10.1101/cshperspect.a011866.
PMID: 25420283
Rampton D, Folkersen J, Fishbane S, Hedenus M, Howaldt S, Locatelli F, Patni S, Szebeni J, Weiss G: Hypersensitivity reactions to intravenous iron: guidance for risk minimization and management. Haematologica. 2014 Nov;99(11):1671-6. doi: 10.3324/haematol.2014.111492.
PMID: 24310424
Geisser P, Burckhardt S: The pharmacokinetics and pharmacodynamics of iron preparations. Pharmaceutics. 2011 Jan 4;3(1):12-33. doi: 10.3390/pharmaceutics3010012.
PMID: 8985284
Adams PC, Deugnier Y, Moirand R, Brissot P: The relationship between iron overload, clinical symptoms, and age in 410 patients with genetic hemochromatosis. Hepatology. 1997 Jan;25(1):162-6. doi: 10.1002/hep.510250130.
PMID: 21452290
Bacon BR, Adams PC, Kowdley KV, Powell LW, Tavill AS: Diagnosis and management of hemochromatosis: 2011 practice guideline by the American Association for the Study of Liver Diseases. Hepatology. 2011 Jul;54(1):328-43. doi: 10.1002/hep.24330.

Link

Contoh Produk & Brand

Produk: 7 • International brands: 0

Produk

Monoferric

Solution • 100 mg / mL • Intravenous • Canada • Approved
Monoferric

Injection, solution • 100 mg/1mL • Intravenous • US • Approved
Monoferric

Injection, solution • 500 mg/5mL • Intravenous • US • Approved
Monoferric

Injection, solution • 1000 mg/10mL • Intravenous • US • Approved
Monoferric

Solution • 100 mg/1mL • Intravenous • US • Approved
Monoferric

Solution • 500 mg/5mL • Intravenous • US • Approved
Monoferric

Solution • 1000 mg/10mL • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.