Peringatan Keamanan

There is no information available regarding the LD50 and overdose of mavorixafor.

Mavorixafor

DB05501

small molecule approved investigational

Deskripsi

Mavorixafor is a CXC chemokine receptor 4 (CXCR4) antagonist.L50642 It was first approved by the FDA on April 30, 2024, for the treatment of warts, hypogammaglobulinemia, infections, and myelokathexis (WHIM) syndrome, a genetic immunodeficiency disorder characterized by a reduced number of mature neutrophils and lymphocytes.L50647 WHIM syndrome is caused by mutations in the CXCR4 gene, which leads to overactivation of CXCR4 signalling pathways.A263652 Mavorixafor prevents the activation of CXCR4.L50642

As CXCR4 mutations have also been implicated in human immunodeficiency virus (HIV), Waldenstrom’s macroglobulinemia (WM), B-cell non-Hodgkin lymphoma, and solid tumours, including melanoma, mavorixafor is being investigated in these conditions.A263632, A263627

Struktur Molekul 2D

Berat 349.482
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 (CV%) terminal half-life was 82 h (34%) following a single-dose administration of mavorixafor 400 mg in healthy subjects.[L50642]
Volume Distribusi Mavorixafor volume of distribution was 768 L in adults with WHIM syndrome.[L50642]
Klirens (Clearance) The mean (CV%) apparent clearance was 62 L/h (40%) following a single-dose administration of mavorixafor 400 mg in healthy subjects. Mavorixafor exhibits at least partial nonlinear apparent clearance; however, this is not clinically significant at the approved recommended dosage.[L50642]

Absorpsi

In adults with WHIM syndrome, the mean (CV%) Cmax at steady-state is 3304 (58.6%) ng/mL and the AUC from 0 to 24 hours (AUC0-24h) is 13970 (58.4%) ngxh/mL following 400 mg once daily.L50642 Mavorixafor demonstrates nonlinear pharmacokinetics with greater than dose-proportional increases in Cmax and AUC0-24h over a dose range of 50 mg (0.125 times the recommended dosage) to 400 mg. Mavorixafor steady-state is reached after approximately 9 to 12 days at the highest approved recommended dosage in healthy subjects. Mavorixafor median (range) Tmax is 2.8 hours (1.9 to 4 hours) at the highest approved recommended dosage. Food decreases Cmax and AUC.L50642

Metabolisme

Mavorixafor is metabolized by CYP3A4 and, to a lesser extent, CYP2D6.L50642

Rute Eliminasi

After a single oral dose of radiolabeled mavorixafor, 74.2% of the administered dose was recovered out of which 61.0% of administered radioactivity was recovered in feces and 13.2% (3% unchanged) was recovered in the urine over the 240-hour collection period in healthy subjects.L50642

Interaksi Makanan

2 Data
  • 1. Take on an empty stomach. Take drug after an overnight fast, 30 minutes before food. Food decreases drug exposure.
  • 2. Take with or without food. Grapefruit may decrease mavorixafor metabolism and increase the risk of drug adverse reactions.

Interaksi Obat

805 Data
Ivabradine The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Ivabradine.
Afatinib The excretion of Mavorixafor can be decreased when combined with Afatinib.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Mavorixafor.
Brentuximab vedotin The metabolism of Brentuximab vedotin can be decreased when combined with Mavorixafor.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Mavorixafor.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Mavorixafor.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Mavorixafor.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Mavorixafor.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Mavorixafor.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Mavorixafor.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Mavorixafor.
Silodosin The excretion of Silodosin can be decreased when combined with Mavorixafor.
Topotecan The excretion of Topotecan can be decreased when combined with Mavorixafor.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Mavorixafor.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Mavorixafor.
Everolimus The excretion of Mavorixafor can be decreased when combined with Everolimus.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Mavorixafor.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Mavorixafor.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Mavorixafor.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Mavorixafor.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Mavorixafor.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Mavorixafor.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Mavorixafor.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Mavorixafor.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Mavorixafor.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Mavorixafor.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Mavorixafor.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Mavorixafor.
Warfarin The metabolism of Warfarin can be decreased when combined with Mavorixafor.
Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Mavorixafor.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Mavorixafor.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Mavorixafor.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Mavorixafor.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Mavorixafor.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Mavorixafor.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Mavorixafor.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Mavorixafor.
Vincristine The metabolism of Vincristine can be decreased when combined with Mavorixafor.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Mavorixafor.
Lumacaftor The metabolism of Mavorixafor can be increased when combined with Lumacaftor.
Dofetilide The metabolism of Dofetilide can be decreased when combined with Mavorixafor.
Citalopram The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Citalopram.
Ziprasidone The metabolism of Mavorixafor can be decreased when combined with Ziprasidone.
Anagrelide The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Anagrelide.
Disopyramide The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Disopyramide.
Clemastine The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Clemastine.
Ibutilide The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Ibutilide.
Valproic acid The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Valproic acid.
Terfenadine The metabolism of Mavorixafor can be decreased when combined with Terfenadine.
Grepafloxacin The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Grepafloxacin.
Quinine The excretion of Mavorixafor can be decreased when combined with Quinine.
Fluoxetine The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Fluoxetine.
Sotalol The metabolism of Sotalol can be decreased when combined with Mavorixafor.
Erlotinib The metabolism of Erlotinib can be decreased when combined with Mavorixafor.
Toremifene The excretion of Mavorixafor can be decreased when combined with Toremifene.
Cisapride The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Cisapride.
Imatinib The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Imatinib.
Astemizole The metabolism of Astemizole can be decreased when combined with Mavorixafor.
Thioridazine The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Thioridazine.
Trovafloxacin The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Trovafloxacin.
Mifepristone The excretion of Mavorixafor can be decreased when combined with Mifepristone.
Flupentixol The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Flupentixol.
Cocaine The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Cocaine.
Quinidine The excretion of Mavorixafor can be decreased when combined with Quinidine.
Procainamide The metabolism of Procainamide can be decreased when combined with Mavorixafor.
Pimozide The metabolism of Pimozide can be decreased when combined with Mavorixafor.
Amiodarone The metabolism of Mavorixafor can be decreased when combined with Amiodarone.
Arsenic trioxide The excretion of Mavorixafor can be decreased when combined with Arsenic trioxide.
Escitalopram The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Escitalopram.
Domperidone The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Domperidone.
Sparfloxacin The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Sparfloxacin.
Halofantrine The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Halofantrine.
Bepridil The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Bepridil.
Paliperidone The excretion of Mavorixafor can be decreased when combined with Paliperidone.
Lithium cation The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Lithium cation.
Temafloxacin The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Temafloxacin.
Zuclopenthixol The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Zuclopenthixol.
Tetrabenazine The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Tetrabenazine.
Dronedarone The metabolism of Mavorixafor can be decreased when combined with Dronedarone.
Nilotinib The metabolism of Mavorixafor can be decreased when combined with Nilotinib.
Vandetanib The excretion of Mavorixafor can be decreased when combined with Vandetanib.
Romidepsin The metabolism of Romidepsin can be decreased when combined with Mavorixafor.
Asenapine The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Asenapine.
Artemether The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Lumefantrine.
Vemurafenib The serum concentration of Mavorixafor can be increased when it is combined with Vemurafenib.
Ribociclib The metabolism of Mavorixafor can be decreased when combined with Ribociclib.
Glasdegib The excretion of Mavorixafor can be decreased when combined with Glasdegib.
Deutetrabenazine The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Deutetrabenazine.
Macimorelin The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Macimorelin.
Terodiline The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Terodiline.
Leuprolide The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Leuprolide.
Goserelin The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Goserelin.
Erythromycin The serum concentration of Mavorixafor can be increased when it is combined with Erythromycin.
Azithromycin The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Azithromycin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Moxifloxacin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Sulfisoxazole.
Amitriptyline The metabolism of Amitriptyline can be decreased when combined with Mavorixafor.
Methadone The risk or severity of QTc prolongation can be increased when Mavorixafor is combined with Methadone.
Diltiazem The metabolism of Mavorixafor can be decreased when combined with Diltiazem.

Target Protein

C-X-C chemokine receptor type 4 CXCR4

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17452489
    Stone ND, Dunaway SB, Flexner C, Tierney C, Calandra GB, Becker S, Cao YJ, Wiggins IP, Conley J, MacFarland RT, Park JG, Lalama C, Snyder S, Kallungal B, Klingman KL, Hendrix CW: Multiple-dose escalation study of the safety, pharmacokinetics, and biologic activity of oral AMD070, a selective CXCR4 receptor inhibitor, in human subjects. Antimicrob Agents Chemother. 2007 Jul;51(7):2351-8. Epub 2007 Apr 23.
  • PMID: 36923305
    Andtbacka RHI, Wang Y, Pierce RH, Campbell JS, Yushak M, Milhem M, Ross M, Niland K, Arbeit RD, Parasuraman S, Bickley K, Yeung CC, Aicher LD, Smythe KS, Gan L: Mavorixafor, an Orally Bioavailable CXCR4 Antagonist, Increases Immune Cell Infiltration and Inflammatory Status of Tumor Microenvironment in Patients with Melanoma. Cancer Res Commun. 2022 Aug 31;2(8):904-913. doi: 10.1158/2767-9764.CRC-22-0090. eCollection 2022 Aug.
  • PMID: 32784523
    Milanesi S, Locati M, Borroni EM: Aberrant CXCR4 Signaling at Crossroad of WHIM Syndrome and Waldenstrom's Macroglobulinemia. Int J Mol Sci. 2020 Aug 8;21(16):5696. doi: 10.3390/ijms21165696.
  • PMID: 32870250
    Dale DC, Firkin F, Bolyard AA, Kelley M, Makaryan V, Gorelick KJ, Ebrahim T, Garg V, Tang W, Jiang H, Skerlj R, Beaussant Cohen S: Results of a phase 2 trial of an oral CXCR4 antagonist, mavorixafor, for treatment of WHIM syndrome. Blood. 2020 Dec 24;136(26):2994-3003. doi: 10.1182/blood.2020007197.
  • PMID: 36089616
    Zmajkovicova K, Pawar S, Maier-Munsa S, Maierhofer B, Wiest I, Skerlj R, Taveras AG, Badarau A: Genotype-phenotype correlations in WHIM syndrome: a systematic characterization of CXCR4(WHIM) variants. Genes Immun. 2022 Sep;23(6):196-204. doi: 10.1038/s41435-022-00181-9. Epub 2022 Sep 12.

Contoh Produk & Brand

Produk: 1 • International brands: 0
Produk
  • Xolremdi
    Capsule, gelatin coated • 100 mg/1 • Oral • US • Approved

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