125I-SDF-CXCR4 ( IC50 = 13 nM ); HIV-1 (NL4.3 strain) ( IC50 = 1 nM ); HIV-1 (NL4.3 strain) ( IC50 = 9 nM ); HIV-1 (NL4.3 strain) ( IC50 = 3 nM ); HIV-1 (NL4.3 strain) ( IC50 = 26 nM )

AMD-070 shows promising oral bioavailability in rat and dog. The rate of clearance is species dependent with AMD-070 having lower clearance in dog compared to rat.

Absorption
In adults with WHIM syndrome, after a once-daily dose of 400 mg, the steady-state mean (CV%) Cmax was 3304 (58.6%) ng/mL, and the 0-24 hour AUC (AUC0-24h) was 13970 (58.4%) ng·h/mL. The pharmacokinetics of Mavorixafor are non-linear; the increases in Cmax and AUC0-24h are greater than dose-proportional across the dose range of 50 mg (0.125 times the recommended dose) to 400 mg. In healthy subjects, steady-state plasma concentrations of Mavorixafor are reached approximately after 9 to 12 days following administration of the highest approved recommended dose. At the highest approved recommended dose, the median (range) Tmax of Mavorixafor is 2.8 hours (1.9 to 4 hours). Food decreases Cmax and AUC.
Excretion Route
In healthy subjects, following a single oral dose of radiolabeled mavolixafor, 74.2% of the administered dose was recovered within a 240-hour collection period, with 61.0% of the radioactive material recovered in feces and 13.2% (3% unchanged) in urine.
Volume of Distribution
In adults with WHIM syndrome, the volume of distribution of mavolixafor is 768 L.
Clearance
In healthy subjects, following a single dose of 400 mg mavolixafor, the mean (coefficient of variation) apparent clearance was 62 L/h (40%). Mavolixafor exhibits at least partially nonlinear apparent clearance; however, this nonlinear clearance is not clinically significant at the approved recommended dose.
Protein Binding
In vitro studies have shown that mavolixafor binds to human plasma proteins >93%.
Metabolism/Metabolites
Mavolixafor is primarily metabolized via CYP3A4, and secondarily via CYP2D6.
Biological Half-Life
In healthy subjects, the mean (CV%) terminal half-life after a single dose of 400 mg mavolixafor is 82 hours (34%).
Mavorixafor (AMD070) is a small molecule drug with high oral bioavailability; good oral bioavailability was observed in both rats and dogs [1]
- In CD-1 mice, after oral administration of 400 μg/mouse of Mavorixafor (AMD070), the drug was detected in lung tissue, and its concentration varied over time. EC₉₀ (44 ng/mL) was used as the reference threshold for pharmacodynamic activity [2]
- In C57BL/6 mice, after intraperitoneal injection of Mavorixafor (AMD070), the drug was distributed in plasma, liver, and lung tissue, and its concentration was detected at different time points [2]

Mavorixafor (AMD070) showed no cytotoxicity to MT-4 cells and PBMCs at in vitro concentrations exceeding 23 μM[1]
Effects during pregnancy and lactation
◉ Overview of use during lactation
There is currently no information regarding the use of mavorixafor during lactation. The manufacturer recommends against breastfeeding during treatment and for three weeks after the last dose.
◉ Effects on breastfed infants
No published information was found as of the revision date.
◉ Effects on lactation and breast milk
No published information was found as of the revision date.

PLoS One.2016 Mar 21;11(3):e0151765;J Med Chem.2010 Apr 22;53(8):3376-88.

Mavorixafor is a CXC chemokine receptor 4 (CXCR4) antagonist. It was first approved by the FDA on April 30, 2024, for the treatment of warts, hypogammaglobulinemia, infection, and bone marrow retention (WHIM) syndrome. WHIM syndrome is a inherited immunodeficiency disorder characterized by a decrease in the number of mature neutrophils and lymphocytes. WHIM syndrome is caused by mutations in the CXCR4 gene, leading to overactivation of the CXCR4 signaling pathway. Mavorixafor inhibits CXCR4 activation. Because CXCR4 mutations are also associated with human immunodeficiency virus (HIV), Waldenström macroglobulinemia (WM), B-cell non-Hodgkin lymphoma, and solid tumors including melanoma, Mavorixafor is being investigated in these diseases. Mavorixafor's mechanism of action is as a CXC chemokine receptor 4 antagonist, cytochrome P450 2D6 inhibitor, cytochrome P450 3A4 inhibitor, and P-glycoprotein inhibitor. Mavorixafor is an orally bioavailable CXC chemokine receptor 4 (CXCR4) inhibitor with potential antitumor and immune checkpoint inhibitory activities. After administration, Mavorixafor selectively binds to CXCR4, preventing CXCR4 from binding to its ligand stromal cell-derived factor 1 (SDF-1 or CXCL12). This inhibits receptor activation, leading to reduced proliferation and migration of CXCR4-overexpressing tumor cells. Furthermore, inhibition of CXCR4 prevents the recruitment of regulatory T cells and myeloid-derived suppressor cells (MDSCs) to the tumor microenvironment, thereby eliminating CXCR4-mediated immunosuppression and activating cytotoxic T lymphocyte-mediated immune responses against cancer cells. The G protein-coupled receptor CXCR4 is upregulated in various tumor cell types, inducing the recruitment of immunosuppressive cells to the tumor microenvironment, inhibiting immune surveillance, and promoting tumor angiogenesis and tumor cell proliferation. It is also a co-receptor for HIV entry into T cells. Mavorixafor is a small molecule drug, currently in Phase IV clinical trials (covering all indications), and was first approved in 2024 for the treatment of cancer, with six investigational indications. It is a derivative of AMD3100, a CXCR4 blocker.

C21H28CLN5

385.933523178101

385.203

880549-30-4

558447-26-0;880549-30-4 (HCl); 2309699-17-8

71576687

Light yellow to brown solid at room temperature

5.078

3

4

7

27

431

1

N([C@H]1CCCC2C=CC=NC1=2)(CCCCN)CC1=NC2C=CC=CC=2N1.Cl

DBNMEMJSDAAGNZ-FYZYNONXSA-N

InChI=1S/C21H27N5.ClH/c22-12-3-4-14-26(15-20-24-17-9-1-2-10-18(17)25-20)19-11-5-7-16-8-6-13-23-21(16)19;/h1-2,6,8-10,13,19H,3-5,7,11-12,14-15,22H2,(H,24,25);1H/t19-;/m0./s1

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)