Insulin icodec

DB16693

biotech approved investigational

Deskripsi

Insulin icodec is an ultra long-acting basal insulin analogue. It is a re-engineered version of the ultra long-acting oral basal insulin OI338, with several modifications introduced to significantly extend the half-life.A264093 These modifications - which cause increased serum albumin binding and attenuated insulin receptor affinity - result in a mean half-life of approximately 196 hours, allowing for once-weekly administration.L50758,A263818

Insulin icodec was approved by Health Canada in March 2024 for the treatment of adult patients with type 1 or 2 diabetes mellitus,L50758 and was subsequently approved by the EMA in May 2024 for the same indication.L50763 It has also been approved in Japan and Australia.L51078 In July 2024, the US FDA rejected the approval of insulin icodec, citing concerns regarding hypoglycemia and the indication being sought for type 1 diabetes mellitus.L51078

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean half-life of insulin icodec is approximately 196 hours,[A263818] reported as roughly one week in drug prescribing information.[L50758,L50763]
Volume Distribusi According to population pharmacokinetic modelling, the steady-state volume of distribution of insulin icodec is 9.79 L.[L50758]
Klirens (Clearance) According to population pharmacokinetic modelling, the steady-state mean clearance of insulin icodec is 0.045 L/h.[L50758]

Absorpsi

The time to maximum plasma concentration (Tmax) is approximately 15-18 hours.L50758 Dose proportional increases in Cmax and AUC are observed across the standard dosing range.L50758 Steady-state levels are reached after 2-3 weeks of administration with the one-time 50% additional dose for the first dose, and after 2-4 weeks without the one-time additional dose.L50758

Metabolisme

Insulin icodec, similar to endogenous insulin, is likely metabolized by insulin degrading enzymes.L50758

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Take with or without food. Insulin icodec is a long-acting insulin and therefore does not need to be administered with respect to food.

Interaksi Obat

790 Data
Liraglutide Liraglutide may increase the hypoglycemic activities of Insulin icodec.
Metreleptin Metreleptin may increase the hypoglycemic activities of Insulin icodec.
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Insulin icodec.
Pioglitazone The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin icodec.
Pramlintide Pramlintide may increase the hypoglycemic activities of Insulin icodec.
Rosiglitazone The risk or severity of congestive heart failure can be increased when Insulin icodec is combined with Rosiglitazone.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Insulin icodec.
Edetic acid Edetic acid may increase the hypoglycemic activities of Insulin icodec.
Esmolol Esmolol may increase the hypoglycemic activities of Insulin icodec.
Betaxolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Betaxolol.
Metoprolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Metoprolol.
Atenolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Atenolol.
Timolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Timolol.
Sotalol The risk or severity of hypoglycemia can be increased when Sotalol is combined with Insulin icodec.
Propranolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Propranolol.
Labetalol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Labetalol.
Bisoprolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Bisoprolol.
Alprenolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Alprenolol.
Pindolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Pindolol.
Carvedilol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Carvedilol.
Propafenone The therapeutic efficacy of Insulin icodec can be increased when used in combination with Propafenone.
Acebutolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Acebutolol.
Nadolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Nadolol.
Bevantolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Bevantolol.
Practolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Practolol.
Penbutolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Penbutolol.
Oxprenolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Oxprenolol.
Dexpropranolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Dexpropranolol.
Celiprolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Celiprolol.
Nebivolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Nebivolol.
Bufuralol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Bufuralol.
Bopindolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Bopindolol.
Bupranolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Bupranolol.
Indenolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Indenolol.
Arotinolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Arotinolol.
Levobetaxolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Levobetaxolol.
Talinolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Talinolol.
Anisodamine The therapeutic efficacy of Insulin icodec can be increased when used in combination with Anisodamine.
Landiolol Landiolol may increase the hypoglycemic activities of Insulin icodec.
Bucindolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Bucindolol.
Esatenolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Esatenolol.
Cloranolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Cloranolol.
Mepindolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Mepindolol.
Epanolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Epanolol.
Tertatolol The therapeutic efficacy of Insulin icodec can be increased when used in combination with Tertatolol.
Moxifloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Insulin icodec can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Insulin icodec can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Insulin icodec can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Insulin icodec can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Insulin icodec can be increased when used in combination with Pipemidic acid.
Methyclothiazide The risk or severity of hypoglycemia can be increased when Methyclothiazide is combined with Insulin icodec.
Chlorthalidone The risk or severity of hypoglycemia can be increased when Chlorthalidone is combined with Insulin icodec.
Bendroflumethiazide The risk or severity of hypoglycemia can be increased when Bendroflumethiazide is combined with Insulin icodec.
Metolazone The risk or severity of hypoglycemia can be increased when Metolazone is combined with Insulin icodec.
Benzthiazide The risk or severity of hypoglycemia can be increased when Benzthiazide is combined with Insulin icodec.
Hydroflumethiazide The risk or severity of hypoglycemia can be increased when Hydroflumethiazide is combined with Insulin icodec.
Indapamide The risk or severity of hypoglycemia can be increased when Indapamide is combined with Insulin icodec.
Chlorothiazide The risk or severity of hypoglycemia can be increased when Chlorothiazide is combined with Insulin icodec.
Hydrochlorothiazide The risk or severity of hypoglycemia can be increased when Hydrochlorothiazide is combined with Insulin icodec.
Trichlormethiazide The risk or severity of hypoglycemia can be increased when Trichlormethiazide is combined with Insulin icodec.
Polythiazide The risk or severity of hypoglycemia can be increased when Polythiazide is combined with Insulin icodec.
Quinethazone The risk or severity of hypoglycemia can be increased when Quinethazone is combined with Insulin icodec.
Cyclopenthiazide The risk or severity of hypoglycemia can be increased when Cyclopenthiazide is combined with Insulin icodec.
Epitizide The therapeutic efficacy of Insulin icodec can be decreased when used in combination with Epitizide.
Amitriptyline Amitriptyline may decrease the hypoglycemic activities of Insulin icodec.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Insulin icodec.
Imipramine Imipramine may decrease the hypoglycemic activities of Insulin icodec.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Insulin icodec.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Insulin icodec.
Trimipramine Trimipramine may decrease the hypoglycemic activities of Insulin icodec.
Doxepin Doxepin may decrease the hypoglycemic activities of Insulin icodec.
Desipramine Desipramine may decrease the hypoglycemic activities of Insulin icodec.

Target Protein

Insulin receptor INSR
Insulin-like growth factor 1 receptor IGF1R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 34413118
    Nishimura E, Pridal L, Glendorf T, Hansen BF, Hubalek F, Kjeldsen T, Kristensen NR, Lutzen A, Lyby K, Madsen P, Pedersen TA, Ribel-Madsen R, Stidsen CE, Haahr H: Molecular and pharmacological characterization of insulin icodec: a new basal insulin analog designed for once-weekly dosing. BMJ Open Diabetes Res Care. 2021 Aug;9(1):e002301. doi: 10.1136/bmjdrc-2021-002301.
  • PMID: 33944562
    Kjeldsen TB, Hubalek F, Hjorringgaard CU, Tagmose TM, Nishimura E, Stidsen CE, Porsgaard T, Fledelius C, Refsgaard HHF, Gram-Nielsen S, Naver H, Pridal L, Hoeg-Jensen T, Jeppesen CB, Manfe V, Ludvigsen S, Lautrup-Larsen I, Madsen P: Molecular Engineering of Insulin Icodec, the First Acylated Insulin Analog for Once-Weekly Administration in Humans. J Med Chem. 2021 Jul 8;64(13):8942-8950. doi: 10.1021/acs.jmedchem.1c00257. Epub 2021 May 4.

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