Peringatan Keamanan

There is no human data on the safety of Letemovir in pregnancy.L46807 Embryo-fetal toxicity and malformations have been observed in rats at exposures 11 times the human exposure at the recommended human dose (RHD) of Letemovir. No such toxicity was noted in rats at 3 times human exposure at the RHD or in rabbits at values less than human exposure with the RHD. Total litter loss was observed in 21.7% of female rats at 2 times human exposure at RHD. This did not occur at values similar to human exposure at RHD.

No human data is available regarding lactation.L46807 Letemovir has been observed in the milk of lactating rats and in the blood of their nursing pups.

No data is available concerning the effect of Letemovir on human fertility.L46807 Testicular toxicity leading to reduced fertility has been observed in male rats.

No antidote exists for Letemovir overdosage.L46807 The effectiveness of dialysis in clearing plasma of Letemovir is unknown.

Letermovir

DB12070

small molecule approved investigational

Deskripsi

Letermovir recieved approval from the FDA on November 8th, 2017 for use in prophylaxis of cytomegalovirus (CMV) infection in allogeneic hematopoietic stem cell transplant patients.L1021 It is the first of a new class of CMV anti-infectives called DNA terminase complex inhibitors.A31290 Letermovir has recieved both priority and orphan drug status from the FDA. It is currently marketed under the brand name Prevymis.L1021

Struktur Molekul 2D

Berat 572.561
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean terminal half-life was observed to be 12 hours following administration of Letemovir 480 mg IV once daily.[L46807]
Volume Distribusi The mean steady state volume of distribution is 45.5L.[L46807]
Klirens (Clearance) The mean clearance is 11.25 L/h in healthy subjects.[A31281]

Absorpsi

Letermovir has a bioavailability of 94% in healthy subjects when administered without cyclosporin, 35% in HSCT recipients when administered without cyclosporin, and 85% in HSCT recipients when administered with cyclosporin.L46807 Letermovir's Tmax is 45 min to 2.25 hours.L46807 Time to steady state has been observed to be 9-10 days. Taking Letermovir with food increases Cmax by an average of 129.82% (range of 104.35%-161.50%).L46807 No significant effect on AUC has been observed.

Metabolisme

Letermovir undergoes a minor degree of metabolism through UGT1A1/1A3.L46807

Rute Eliminasi

Letemovir is taken up by the liver through OATP1B1/3 transporters. 93% is excreted in the feces with 70% as the parent drug.L46807 <2% is excreted in the urine.

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. Co-administration may lead to decreased serum concentrations of letermovir.
  • 2. Take with or without food.

Interaksi Obat

521 Data
Pravastatin The excretion of Pravastatin can be decreased when combined with Letermovir.
Diethylstilbestrol The metabolism of Diethylstilbestrol can be decreased when combined with Letermovir.
Indomethacin The metabolism of Letermovir can be decreased when combined with Indomethacin.
Rosiglitazone The metabolism of Rosiglitazone can be decreased when combined with Letermovir.
Cerivastatin The metabolism of Cerivastatin can be decreased when combined with Letermovir.
Diclofenac The metabolism of Diclofenac can be decreased when combined with Letermovir.
Naproxen The metabolism of Naproxen can be decreased when combined with Letermovir.
Disulfiram The metabolism of Disulfiram can be decreased when combined with Letermovir.
Mifepristone The metabolism of Mifepristone can be decreased when combined with Letermovir.
Repaglinide The metabolism of Repaglinide can be decreased when combined with Letermovir.
Ezetimibe The excretion of Ezetimibe can be decreased when combined with Letermovir.
Dipyridamole The excretion of Letermovir can be decreased when combined with Dipyridamole.
Fenofibrate The metabolism of Fenofibrate can be decreased when combined with Letermovir.
Nitrendipine The metabolism of Nitrendipine can be decreased when combined with Letermovir.
Rosuvastatin The metabolism of Rosuvastatin can be decreased when combined with Letermovir.
Nifedipine The metabolism of Nifedipine can be decreased when combined with Letermovir.
Nefazodone The excretion of Letermovir can be decreased when combined with Nefazodone.
Clarithromycin The metabolism of Clarithromycin can be decreased when combined with Letermovir.
Taurocholic acid The excretion of Letermovir can be increased when combined with Taurocholic acid.
Prasterone sulfate The metabolism of Prasterone sulfate can be decreased when combined with Letermovir.
Benzbromarone The excretion of Letermovir can be decreased when combined with Benzbromarone.
Dihydroergocristine The metabolism of Dihydroergocristine can be decreased when combined with Letermovir.
Belantamab mafodotin The excretion of Belantamab mafodotin can be decreased when combined with Letermovir.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Letermovir.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Letermovir.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Letermovir.
Colchicine The metabolism of Colchicine can be decreased when combined with Letermovir.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Letermovir.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Letermovir.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Letermovir.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Letermovir.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Letermovir.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Letermovir.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Letermovir.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Letermovir.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Letermovir.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Letermovir.
Cephalexin The metabolism of Cephalexin can be decreased when combined with Letermovir.
Levocarnitine The excretion of Letermovir can be decreased when combined with Levocarnitine.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Letermovir.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Letermovir.
Saxagliptin The metabolism of Saxagliptin can be decreased when combined with Letermovir.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Letermovir.
Estradiol The metabolism of Estradiol can be decreased when combined with Letermovir.
Conjugated estrogens The excretion of Letermovir can be decreased when combined with Conjugated estrogens.
Hydrocortisone The metabolism of Hydrocortisone can be decreased when combined with Letermovir.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Letermovir.
Dexamethasone The metabolism of Dexamethasone can be decreased when combined with Letermovir.
Sitagliptin The metabolism of Sitagliptin can be decreased when combined with Letermovir.
Tenofovir alafenamide The metabolism of Tenofovir alafenamide can be decreased when combined with Letermovir.
Dexamethasone acetate The metabolism of Dexamethasone acetate can be decreased when combined with Letermovir.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Letermovir.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Letermovir.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Letermovir.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Letermovir.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Letermovir.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Letermovir.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Letermovir.
Desogestrel The metabolism of Letermovir can be increased when combined with Desogestrel.
Zidovudine The metabolism of Letermovir can be increased when combined with Zidovudine.
Lamotrigine The metabolism of Letermovir can be increased when combined with Lamotrigine.
Efavirenz The metabolism of Letermovir can be increased when combined with Efavirenz.
Primidone The metabolism of Letermovir can be increased when combined with Primidone.
Testosterone propionate The metabolism of Letermovir can be increased when combined with Testosterone propionate.
Nelfinavir The metabolism of Letermovir can be increased when combined with Nelfinavir.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Letermovir.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Letermovir.
Chlorpromazine The metabolism of Chlorpromazine can be decreased when combined with Letermovir.
Ketoconazole The metabolism of Letermovir can be decreased when combined with Ketoconazole.
Fusidic acid The excretion of Letermovir can be decreased when combined with Fusidic acid.
Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Letermovir.
Imipramine The metabolism of Imipramine can be increased when combined with Letermovir.
Terfenadine The metabolism of Terfenadine can be decreased when combined with Letermovir.
Ritonavir The metabolism of Letermovir can be increased when combined with Ritonavir.
Tipranavir The metabolism of Letermovir can be increased when combined with Tipranavir.
Quinine The metabolism of Quinine can be decreased when combined with Letermovir.
Chloroquine The metabolism of Chloroquine can be decreased when combined with Letermovir.
Asunaprevir The metabolism of Asunaprevir can be decreased when combined with Letermovir.
Clozapine The serum concentration of Clozapine can be increased when it is combined with Letermovir.
Panobinostat The serum concentration of Panobinostat can be increased when it is combined with Letermovir.
Celecoxib The metabolism of Celecoxib can be decreased when combined with Letermovir.
Terbinafine The metabolism of Terbinafine can be decreased when combined with Letermovir.
Nicardipine The metabolism of Nicardipine can be decreased when combined with Letermovir.
Halofantrine The metabolism of Halofantrine can be decreased when combined with Letermovir.
Cisapride The metabolism of Cisapride can be decreased when combined with Letermovir.
Raloxifene The excretion of Raloxifene can be decreased when combined with Letermovir.
Sulfasalazine The excretion of Letermovir can be decreased when combined with Sulfasalazine.
Teriflunomide The excretion of Letermovir can be decreased when combined with Teriflunomide.
Riociguat The metabolism of Riociguat can be decreased when combined with Letermovir.
Fimasartan The excretion of Fimasartan can be decreased when combined with Letermovir.
Revefenacin Letermovir may decrease the excretion rate of Revefenacin which could result in a higher serum level.
Darolutamide The excretion of Letermovir can be decreased when combined with Darolutamide.
Tazemetostat The metabolism of Tazemetostat can be decreased when combined with Letermovir.
Gefitinib The metabolism of Gefitinib can be decreased when combined with Letermovir.
Ivermectin The excretion of Letermovir can be decreased when combined with Ivermectin.
Testosterone The metabolism of Testosterone can be decreased when combined with Letermovir.
Sumatriptan The excretion of Sumatriptan can be decreased when combined with Letermovir.
Mycophenolate mofetil The metabolism of Mycophenolate mofetil can be decreased when combined with Letermovir.
Apixaban The metabolism of Apixaban can be decreased when combined with Letermovir.
Velpatasvir The metabolism of Velpatasvir can be decreased when combined with Letermovir.

Target Protein

CMV DNA Terminase Complex TRM1

Referensi & Sumber

Synthesis reference: Humphrey GR, Dalby SM, Andreani T, Xiang B, Luzung MR, Song ZJ, Shevlin M, Christensen M, Belyk KM, Tschaen DM. 2016.Asymmetric Synthesis of Letermovir Using a Novel Phase-Transfer Catalyzed Aza-Michael Reaction. Org. Process Res. Dev. 20(6), 1097-1103. DOI: 10.1021/acs.oprd.6b00076
Artikel (PubMed)
  • PMID: 28345163
    Kropeit D, Scheuenpflug J, Erb-Zohar K, Halabi A, Stobernack HP, Hulskotte EGJ, van Schanke A, Zimmermann H, Rubsamen-Schaeff H: Pharmacokinetics and safety of letermovir, a novel anti-human cytomegalovirus drug, in patients with renal impairment. Br J Clin Pharmacol. 2017 Sep;83(9):1944-1953. doi: 10.1111/bcp.13292. Epub 2017 May 5.
  • PMID: 21752907
    Goldner T, Hewlett G, Ettischer N, Ruebsamen-Schaeff H, Zimmermann H, Lischka P: The novel anticytomegalovirus compound AIC246 (Letermovir) inhibits human cytomegalovirus replication through a specific antiviral mechanism that involves the viral terminase. J Virol. 2011 Oct;85(20):10884-93. doi: 10.1128/JVI.05265-11. Epub 2011 Jul 13.
  • PMID: 26345608
    Melendez DP, Razonable RR: Letermovir and inhibitors of the terminase complex: a promising new class of investigational antiviral drugs against human cytomegalovirus. Infect Drug Resist. 2015 Aug 5;8:269-77. doi: 10.2147/IDR.S79131. eCollection 2015.
  • PMID: 29107686
    Chou S: A third component of the human cytomegalovirus terminase complex is involved in letermovir resistance. Antiviral Res. 2017 Dec;148:1-4. doi: 10.1016/j.antiviral.2017.10.019. Epub 2017 Oct 28.
  • PMID: 28356534
    Neuber S, Wagner K, Goldner T, Lischka P, Steinbrueck L, Messerle M, Borst EM: Mutual Interplay between the Human Cytomegalovirus Terminase Subunits pUL51, pUL56, and pUL89 Promotes Terminase Complex Formation. J Virol. 2017 May 26;91(12). pii: e02384-16. doi: 10.1128/JVI.02384-16. Print 2017 Jun 15.

Contoh Produk & Brand

Produk: 14 • International brands: 0
Produk
  • Prevymis
    Solution • 20 mg / mL • Intravenous • Canada • Approved
  • Prevymis
    Tablet • 240 mg • Oral • Canada • Approved
  • Prevymis
    Tablet • 480 mg • Oral • Canada • Approved
  • Prevymis
    Solution • 20 mg / mL • Intravenous • Canada • Approved
  • Prevymis
    Pellet • 20 mg/1 • Oral • US • Approved
  • Prevymis
    Pellet • 120 mg/1 • Oral • US • Approved
  • Prevymis
    Tablet, film coated • 240 mg/1 • Oral • US • Approved
  • Prevymis
    Tablet, film coated • 480 mg/1 • Oral • US • Approved
Menampilkan 8 dari 14 produk.

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