Posaconazole
Synonym(s):;Posaconazole solution;Sch 56592
- CAS NO.:171228-49-2
- Empirical Formula: C37H42F2N8O4
- Molecular Weight: 700.78
- MDL number: MFCD00941162
- EINECS: 682-747-8
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-06-07 16:07:22
What is Posaconazole?
Absorption
Posaconazole is absorbed with a median Tmax of approximately 3 to 5 hours.
Toxicity
During the clinical trials, some patients received posaconazole up to 1600 mg/day with no adverse events noted that were different from the lower doses. In addition, accidental overdose was noted in one patient who took 1200 mg BID for 3 days. No related adverse events were noted by the investigator.
Description
Posaconazole, launched in the UK, is the newest member of the azole class of antifungal agents to reach the market. It is indicated for the treatment and prophylaxis of a range of invasive fungal infections, including aspergillosis,fusariosis, chromoblastomycosis, mycetoma, and coccidiomycosis in patients who are refractory to, or intolerant of, standard therapy with amphotericin B and/or itraconazole. In the US, it is approved for the prophylaxis of invasive Aspergillus and Candida infections in patients 13 years of age who are at high risk of developing these infections due to being severely immunocompromised. Additionally, it is approved for the treatment of oropharyngeal candidiasis. Posaconazole has an expanded spectrum of activity over other members of the azole antifungals. In addition to potent activity against refractory cases of aspergillosis and fluconazole-resistant Candida, it demonstrates activity against Zygomycetes.
The Uses of Posaconazole
Posaconazole is a sterol C14ɑ demethylase inhibitor with an IC50 of 0.25 nM
Background
Posaconazole is a triazole antifungal drug that is used to treat invasive infections by Candida species and Aspergillus species in severely immunocompromised patients.
Indications
Posaconazole is prescribed for the prophylaxis of invasive Aspergillus and Candida infections in patients aged 13 years and older who face a high risk of developing these infections due to severe immunocompromise. This includes individuals undergoing procedures such as hematopoietic stem cell transplant (HSCT) with graft-versus-host disease (GVHD) or those with hematologic malignancies experiencing prolonged neutropenia from chemotherapy. Additionally, it is indicated for the treatment of oropharyngeal candidiasis, including cases refractory to itraconazole and/or fluconazole. Posaconazole serves as an alternative treatment for invasive aspergillosis, Fusarium infections, and zygomycosis in patients intolerant of or with diseases refractory to other antifungals, offering a therapeutic option for challenging fungal infections.
What are the applications of Application
Posaconazole is a triazole anti-fungal
Pharmacokinetics
Posaconazole is an antifungal agent structurally related to itraconazole. It is a drug derived from itraconzaole through the replacement of the chlorine substituents with flourine in the phenyl ring, as well as hydroxylation of the triazolone side chain. These modifications enhance the potency and spectrum of activity of the drug. Posaconazole can be either fungicial or fungistatic in action.
Metabolism
Posaconazole primarily circulates as the parent compound in plasma. Of the circulating metabolites, the majority are glucuronide conjugates formed via UDP glucuronidation (phase 2 enzymes). Posaconazole does not have any major circulating oxidative (CYP450 mediated) metabolites. The excreted metabolites in urine and feces account for ~17% of the administered radiolabeled dose.
Properties of Posaconazole
Melting point: | 170-1720C |
Boiling point: | 850.7±75.0 °C(Predicted) |
Density | 1.36±0.1 g/cm3(Predicted) |
Flash point: | 9℃ |
storage temp. | -20°C |
solubility | Chloroform (Slightly), Methanol (Slightly) |
form | powder |
color | white to beige |
Safety information for Posaconazole
Signal word | Danger |
Pictogram(s) |
Flame Flammables GHS02 Skull and Crossbones Acute Toxicity GHS06 Health Hazard GHS08 |
GHS Hazard Statements |
H225:Flammable liquids H370:Specific target organ toxicity, single exposure |
Precautionary Statement Codes |
P210:Keep away from heat/sparks/open flames/hot surfaces. — No smoking. P260:Do not breathe dust/fume/gas/mist/vapours/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P311:Call a POISON CENTER or doctor/physician. P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. |
Computed Descriptors for Posaconazole
InChIKey | RAGOYPUPXAKGKH-XAKZXMRKSA-N |
SMILES | [C@]1(OC[C@@H](COC2C=CC(N3CCN(C4=CC=C(N5C=NN([C@@H](CC)[C@@H](O)C)C5=O)C=C4)CC3)=CC=2)C1)(CN1N=CN=C1)C1=CC=C(F)C=C1F |&1:0,3,22,25,r| |
Abamectin manufacturer
Prajna generics pvt ltd
SGMR PHARMACEUTICALS PVT LTD
Dr. Reddy's Laboratories Ltd
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