Name | Cancidas |
Synonyms | Cancidas (3S,6S,9S,11R,15S,18S,20R,21S,24S,25S)-21-(2-Aminoethylamino)-3-[3-amino-1(R)-hydroxypropyl]-6-[1(S),2(S)-dihydroxy-2-(4-hydroxyphenyl)ethyl]-18-(10,12-dimethyltetradecanamido)-11,20,25-trihydroxy-15-[1(R)-hydroxyethyl]-1,4,7,13,16,22-hexaazatricyclo[22.3.0.0(9,13)]heptacosane-2,5,8,14,17,23-hexaone diacetate |
CAS | 179463-17-3 |
EINECS | 605-859-0 |
InChI | InChI=1/C52H88N10O15.2C2H4O2/c1-5-28(2)24-29(3)12-10-8-6-7-9-11-13-39(69)56-34-26-38(68)46(55-22-21-54)60-50(75)43-37(67)19-23-61(43)52(77)41(36(66)18-20-53)58-49(74)42(45(71)44(70)31-14-16-32(64)17-15-31)59-48(73)35-25-33(65)27-62(35)51(76)40(30(4)63)57-47(34)72;2*1-2(3)4/h14-17,28-30,33-38,40-46,55,63-68,70-71H,5-13,18-27,53-54H2,1-4H3,(H,56,69)(H,57,72)(H,58,74)(H,59,73)(H,60,75);2*1H3,(H,3,4)/t28?,29?,30-,33-,34-,35+,36-,37+,38-,40+,41+,42+,43?,44+,45+,46+;;/m1../s1 |
InChIKey | OGUJBRYAAJYXQP-LLXMLGLCSA-N |
Molecular Formula | C54H92N10O17 |
Molar Mass | 1153.38 |
Melting Point | >105°C (dec.) |
Boling Point | 1408.1°C at 760 mmHg |
Flash Point | 805.4°C |
Solubility | H2O: soluble15mg/mL (clear solution) |
Vapor Presure | 0mmHg at 25°C |
Appearance | powder |
Color | white to beige |
Storage Condition | -20°C |
In vitro study | Caspofungin acetate is the first new antifungal agent that inhibits the synthesis of β (1,3)-d-glucan, a major component of the cell wall of filamentous fungi. Previous studies have shown that the in vitro activity of caspofungin acetate is tested for antifungal susceptibility of Candida spp. Using standard methods, including Microdilution or heavy dilution, which consists of a variety of Candida spp, establishment of standard 1997 guidelines for the National Committee Clinical Laboratory, including Candida krusei. Although caspofungin acetate is only approved by the FDA for the treatment of aspergillosis, there is information that many species of Candida are sensitive to it. The minimum inhibitory concentrations of Caspofungin acetate against 90% of Candida spp. Were as follows: C. C. Albicans 0.5 μg/mL (range, 0.25-0.5), C. C. Glabrata 1.0 μg/mL (range, 0.25-2.0), C. C. Tropicalis 1.0 μg/mL (range, 0.25-1.0), C. Candida parassilosis 0.5 μg/mL (range, 0.25-1.0), and C. C. Krusei 2.0 μg/mL (range, 0.5-2.0). |
WGK Germany | 3 |
RTECS | TP8046500 |
Reference Show more | 1. Zhan Xin Wu Shiheng Deng Lin Zhang Hongyue Gao Fusheng. Effect of 17-AAG combined with caspofungin on invasive pulmonary aspergillosis in neutrophil deficient rats [J]. Chinese medicine guide 2019 16(10):16-19. 2. Hu Tangling, Shi Gaoxiang, Xu Zhiqing, et al. Inhibitory effect of n-butanol extract from Pulsatilla Decoction on cell wall of Candida albicans [J]. Chinese Journal of Mycology, 2018, 13(05):10-15. 3. Yang Yu, Wang Yadong, Wang Yan, Xu Zhiqing, Wu Daqiang, Wang Tianming, Shao Jing, Wang Changzhong. Effect of Berberine Hydrochloride on Cell Wall Integrity of Candida Albicans in Mycelial Phase [J]. Chinese Journal of Traditional Chinese Medicine, 2021,46(01):155-161. |
use | caspofungin acetate for injection can be used for empirical treatment of neutropenia, suspected fungal infections in patients with fever and invasive aspergillosis that is ineffective or intolerable to other treatments. Caspofungin is effective against Aspergillus (including Aspergillus fumigatus, Aspergillus flavus, Aspergillus nidulans, Aspergillus teruans, Aspergillus terreus and Aspergillus albicans) and Candida (including Candida albicans, Candida Dublin, Candida glabracilli, Candida milkis, Candida crusty, Candida lisolysa, Candida Portugal, Candida parapis, Candida pleata and Candida tropicalis) has in vitro activity. |
pharmacological action | caspofungin acetate is a semi-synthetic lipopeptide (echinocandin) compound synthesized from Glarea Lozoyensis fermentation products. The synthesis of β(1,3)-D-glucan, a basic component of the cell wall of many filamentous fungi and yeasts. P(1,3) -D-glucan is absent in the cells of mammals. In vitro pharmacological studies show that caspofungin has antibacterial activity against many pathogenic Aspergillus and Candida fungi. At present, no standard drug sensitivity test method has been established for the detection of β(1,3)-D-glucan synthesis inhibitors. Moreover, the results of drug sensitivity tests are not necessarily related to clinical results. In mice and rats, the LD50 of caspofungin is approximately between 25mg/kg and 50mg/kg by intravenous injection. No long-term studies have been conducted in animals to assess the possibility of caspofungin carcinogenesis. In mice and rats, the LD50 of caspofungin is approximately between 25mg/kg and 50mg/kg by intravenous injection. Long-term studies have not been conducted in animals to assess the possibility of caspofungin causing cancer. In a series of in vitro studies, caspofungin was not found to be mutagenic or genotoxic. In addition, in the bone marrow chromosome test conducted in mice, when the intravenous dose of caspofungin was as high as 12.5 mg/kg, no genotoxicity was found. |
adverse reactions | ▼ ▲ common general conditions fever, headache, abdominal pain, pain, chills (>1/100) gastrointestinal nausea, diarrhea, vomiting elevated liver liver enzyme levels (aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, direct bilirubin and total bilirubin) renal serum creatinine increased blood anemia (decreased hemoglobin and hematocrit) cardiac tachycardia peripheral vascular phlebitis/thrombophlebitis, intravenous infusion complications, redness respiratory system dyspnea skin rash, pruritus, sweating |
precautions | allergic reactions have been reported during the use of this product. If allergic symptoms occur, the use of this product should be stopped and appropriate treatment should be carried out. Reported adverse reactions that may be mediated by histamine, including rash, facial swelling, angioedema, itching, warmth or bronchospasm, may require discontinuation of treatment with this product and/or appropriate management. [medication for pregnant women and lactating women] pregnant women there is no clinical data on the use of caspofungin in pregnant women. In rats, when a toxic dose of 5mg /kg per day was given to the mother, caspofungin caused a decrease in fetal rat weight and increased the incidence of incomplete ossification of the head and trunk. In addition, at this dose, the incidence of cervical ribs in rats increased. Animal tests have found that caspofen can cross the placental barrier. Unless necessary, this product must not be used during pregnancy. Breastfeeding women It is not clear whether this drug can be excreted by human milk. Therefore, women receiving this product should not breastfeed. [Children's medication] Adequate and well-controlled adult research results, pharmacokinetics data of children patients, and prospective research data on the following indications (see indications) carried out in children patients aged 3 months to 17 years support the safety and effectiveness of this product in children patients aged 3 months to 17 years: For fever, empirical treatment of patients with neutropenia and suspected fungal infection. Treatment of invasive candidiasis, including candidemia, in patients with neutropenia or non-neutropenia. Treatment of esophageal candidiasis. Treatment of patients with refractory or aggressive aspergillosis who cannot tolerate other therapies. Prospective clinical trials on the effectiveness and safety of this product have not been fully studied in newborns and infants under 3 months of age. This product has not been studied in children with endocarditis, osteomyelitis and meningitis caused by Candida. As the initial treatment of invasive aspergillosis in children, this product has not been studied. [medication for elderly patients] compared with healthy young men, the plasma concentration of caspofungin in healthy elderly men and women (65 years old or over) increased slightly (AUC increased by about 28%). The same effect of age differences in older people versus younger people was also found in patients treated with empirical or invasive candidiasis. Elderly patients (65 years or older) do not need to adjust the drug dose. |
biological activity | Caspofungin Acetate (MK-0991, L-743872) is a lipopeptide antifungal β-1,3-glucan synthase inhibitor. |
Target | Value |