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Purity: ≥98%
Rezafungin acetate (Biafungin; CD101 acetate; SP-3025 acetate; Rezzayo) is a novel, broad-spectrum, and long-lasting echinocandin with antifungal activity against Candida spp., Aspergillus spp., and Pneumocystis spp and subsets of echinocandin-resistant Candida auris and azole-resistant Aspergillus isolates. It is chemically related with anidulafungin, and acts as a 1,3-β-D-glucan synthase inhibitor. In Mar 2023, it has been approved by FDA for the treatment of Candidiasis.
| Targets |
1,3-β-D-glucan synthase enzyme complex in the cell walls of fungi
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|---|---|
| ln Vitro |
Rezafungin is an echinocandin antifungal drug. It inhibits the 1,3-β-D-glucan synthase enzyme complex present in the cell walls of fungi, responsible for the formation of 1,3-β-D-glucan. Since 1,3-β-D-glucan is an essential component of fungal cell walls, rezafungin disrupts the cell wall of fungal species, including _Candida_ spp., and acts as a concentration-dependent _in vitro_ fungicidal. Mammalian cells do not express β-1-3-glucan synthase; therefore, the action of rezafungin is specific to fungi. Rezafungin is a member of the family of echinocandins that inhibits 1,3-beta-D-glucan synthase.
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| ln Vivo |
In a mouse infection model, rezafunginacetate (Biafunginacetate) (1 mg/kg; i.p. once daily for 6 days) has demonstrated efficient in vivo prophylaxis against Pneumocystis jiroveci [1].
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| Animal Protocol |
Animal/Disease Models: C3H/HeN mice [1]
Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 6 days Experimental Results: The burden of cell nuclei and ascus was Dramatically diminished. |
| ADME/Pharmacokinetics |
Absorption
Rezafungin dosage ranges from 50 mg (equivalent to 0.125 times the maximum recommended loading dose) to 400 mg, with both Cmax and AUC increasing proportionally with the dose, regardless of whether it is a single or multiple dose. In patients with candidemia and invasive candidiasis, an initial loading dose of 400 mg rezafungin, followed by weekly 200 mg doses, resulted in Cmax of 19.2 mcg/mL, AUC0-168 (AUC0-168) of 0-168 hours post-dose, and Cmin of 2.4 mcg/mL on day 1. In the same cohort, Cmax, AUC0-168, and Cmin of day 15 were 11.8 mcg/mL, 667 mcg/mL, and 2.2 mcg/mL, respectively. Compared with healthy subjects, patients with candidemia had reduced AUC0-168 and Cmax by 30% and 19%, respectively. Age, sex, race, weight, and hepatic impairment had no clinically significant effect on the pharmacokinetics of rezafenib. Elimination Route Rizafenib is primarily excreted in feces. In healthy subjects, 74.3% of the drug was primarily excreted in feces as rezafenib, while 25.7% was primarily excreted in urine as inactive metabolites of rezafenib. Volume of Distribution The volume of distribution of rezafenib is 67 L. Clearance The clearance of rezafenib is 0.35 L/hr. Protein Binding Rizafenib has a high protein binding rate. Protein binding in patients increased from 87.5% to 93.6%, and in healthy adults from 95.6% to >98.6%. Metabolism/Metabolites Rizafenone is metabolized via hydroxylation of the terphenylpentyl ether side chain, producing three hydroxylated metabolite isomers: 2'-, 3'-, or 4'-hydroxypentylrezafenone. Rizafenone can also lose the pentyl group via O-dealkylation to produce depentylrezafenone. Subsequent binding (sulfation) reactions of the hydroxyl metabolites are minimal. Rizafenone is not metabolized in the liver and is not expected to become a clinically relevant substrate for CYP450 enzymes. Biological Half-Life The terminal half-life of rizafenone is 152 hours. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation There is currently no information regarding the use of rezafenamic acid during lactation. Because rezafenamic acid binds to plasma proteins at a rate of approximately 90% and has low oral bioavailability, it is unlikely to enter breast milk and be absorbed by the infant. If the mother needs to use rezafenamic acid, breastfeeding should not be discontinued. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. |
| References |
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| Additional Infomation |
Rezafungin is an echinocandin antibiotic that inhibits 1,3-β-D-glucan synthase. Developed by Cidara Therapeutics, it is approved for the treatment of candidemia and invasive candidiasis in patients aged 18 years and older with limited alternative treatment options. Rezafungin is an echinocandin antifungal drug, belonging to the quaternary ammonium ion class of antibiotics, and is also a nitrogen-containing macrocyclic compound, homocyclic peptide, and aromatic ether compound. Rezafungin is a new generation of semi-synthetic cyclic lipopeptide and echinocandin derivative with potential antifungal activity. After administration, rezafungin inhibits the fungal-specific enzyme 1,3-β-D-glucan synthase (which is crucial for fungal cell wall synthesis), resulting in reduced β(1,3)-D-glucan synthesis. This weakens the fungal cell wall, leading to osmotic lysis, fungal cell wall rupture, and fungal cell death. See also
Rezafenamic acid is an echinocandin antifungal drug. Unlike other echinocandins (such as caspofungin and micafungin), rezafenamic acid has long-acting pharmacokinetics and high stability, allowing for extended dosing intervals and thus maintaining higher plasma exposure. Rezafenamic acid has a half-life exceeding 130 hours, allowing for once-weekly dosing instead of daily dosing. It can only be administered intravenously and does not reach therapeutic concentrations in the central nervous system, eyes, or urine. Rezafenamic acid is effective against Candida albicans, Candida glabrata, Candida parapsilosis, and Candida tropicalis, as well as other Candida and Aspergillus species. Clinical studies have shown that rezafenamic acid is non-inferior to caspofungin in the treatment of candidemia and invasive candidiasis. In March 2023, the U.S. Food and Drug Administration (FDA) approved rezafenamic acid injection for the treatment of candidemia and invasive candidiasis in adults with no other treatment options or limited treatment regimens. In November of the same year, the EU also approved the drug for marketing. |
| Molecular Formula |
C65H88N8O19
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|---|---|
| Molecular Weight |
1285.43643856049
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| Exact Mass |
1225.602
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| Elemental Analysis |
C, 60.73; H, 6.90; N, 8.72; O, 23.65
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| CAS # |
1631754-41-0
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| Related CAS # |
Rezafungin;1396640-59-7
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| PubChem CID |
78318119
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| Appearance |
White to off-white solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
88
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| Complexity |
2300
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| Defined Atom Stereocenter Count |
15
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| SMILES |
CCCCCOC1=CC=C(C=C1)C2=CC=C(C=C2)C3=CC=C(C=C3)C(=O)N[C@H]4C[C@H]([C@H](NC(=O)[C@@H]5[C@H]([C@H](CN5C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]6C[C@H](CN6C(=O)[C@@H](NC4=O)[C@@H](C)O)O)[C@@H]([C@H](C7=CC=C(C=C7)O)O)O)[C@@H](C)O)C)O)OCC[N+](C)(C)C)O
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| InChi Key |
MXMWJAPNUIKPGF-DPHATNFGSA-N
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| InChi Code |
InChI=1S/C63H84N8O17.C2H4O2/c1-8-9-10-28-87-45-25-21-40(22-26-45)38-13-11-37(12-14-38)39-15-17-42(18-16-39)56(80)64-46-31-48(76)61(88-29-27-71(5,6)7)68-60(84)52-53(77)34(2)32-70(52)63(86)50(36(4)73)66-59(83)51(55(79)54(78)41-19-23-43(74)24-20-41)67-58(82)47-30-44(75)33-69(47)62(85)49(35(3)72)65-57(46)811-2(3)4/h11-26,34-36,44,46-55,61,72-73,75-79H,8-10,27-33H2,1-7H3,(H5-,64,65,66,67,68,74,80,81,82,83,84)1H3,(H,3,4)/t34-,35+,36+,44+,46-,47-,48+,49?,50-,51?,52-,53-,54-,55-,61+/m0./s1
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| Chemical Name |
2-(((2R,9S,11R,12R,14aS,15S,16S,20S,25aS)-23-((1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl)-2,11,15-trihydroxy-6,20-bis((R)-1-hydroxyethyl)-16-methyl-5,8,14,19,22,25-hexaoxo-9-(4''-(pentyloxy)-[1,1'
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| Synonyms |
Rezafungin; Rezzayo; Biafungin; SP-3025; 1396640-59-7; Rezafungin ion; Rezafungin cation; CD-101SP; 3025 CD101; SP3025; CD 101.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~230 mg/mL (~178.93 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.75 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5.75 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 5.75 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7779 mL | 3.8897 mL | 7.7794 mL | |
| 5 mM | 0.1556 mL | 0.7779 mL | 1.5559 mL | |
| 10 mM | 0.0778 mL | 0.3890 mL | 0.7779 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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