Biapenem

CAS# 120410-24-4

Biapenem

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Biapenem

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Chemical Properties of Biapenem

Cas No. 120410-24-4 SDF Download SDF
PubChem ID 71339 Appearance Powder
Formula C15H18N4O4S M.Wt 350.39
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Omegacin
Solubility H2O : 10 mg/mL (28.54 mM; Need ultrasonic)
Chemical Name (4R,5S,6S)-3-(6,7-dihydro-5H-pyrazolo[1,2-a][1,2,4]triazol-4-ium-6-ylsulfanyl)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
SMILES CC1C2C(C(=O)N2C(=C1SC3CN4C=NC=[N+]4C3)C(=O)[O-])C(C)O
Standard InChIKey MRMBZHPJVKCOMA-YJFSRANCSA-N
Standard InChI InChI=1S/C15H18N4O4S/c1-7-11-10(8(2)20)14(21)19(11)12(15(22)23)13(7)24-9-3-17-5-16-6-18(17)4-9/h5-11,20H,3-4H2,1-2H3/t7-,8-,10-,11-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Biapenem

DescriptionHighly broad spectrum antibiotic agent. Stable against dehydropeptidase I. Shows bactericidal effects against Gram-negative and Gram-positive aerobic and anaerobic bacteria, including β-lactamase producing species in vivo.

Biapenem Dilution Calculator

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Preparing Stock Solutions of Biapenem

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.854 mL 14.2698 mL 28.5396 mL 57.0793 mL 71.3491 mL
5 mM 0.5708 mL 2.854 mL 5.7079 mL 11.4159 mL 14.2698 mL
10 mM 0.2854 mL 1.427 mL 2.854 mL 5.7079 mL 7.1349 mL
50 mM 0.0571 mL 0.2854 mL 0.5708 mL 1.1416 mL 1.427 mL
100 mM 0.0285 mL 0.1427 mL 0.2854 mL 0.5708 mL 0.7135 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Biapenem

Biapenem is a carbepenem that exhibits antibacterial activities against a wide range of gram-positive and gram-negative bacteria.

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References on Biapenem

PK/PD analysis of biapenem in patients undergoing continuous hemodiafiltration.[Pubmed:26819742]

J Pharm Health Care Sci. 2015 Nov 14;1:31.

BACKGROUND: Continuous hemodiafiltration (CHDF) is used as renal replacement therapy for critically ill patients with renal failure, and to treat hypercytokinemia. Since CHDF also clears therapeutic agents, drug pharmacokinetics (PK) should be dependent upon CHDF conditions. Although the antibiotic Biapenem (BIPM) is used in patients undergoing CHDF, the optimal therapeutic regimen in such patients has not been fully clarified. In this study, we investigated the PK of BIPM in patients with various levels of renal function undergoing CHDF with polysulfone (PS) membrane, and used PK models to identify the optimal administration regimen. METHODS: BIPM (300 mg) was administered by infusion in patients undergoing CHDF (n = 7). Blood and filtrate-dialysate were collected for compartment and non-compartment analysis. RESULTS: The sieving coefficient of PS membrane was 1.00 +/- 0.06 (mean +/- S.D., n = 7), and CHDF clearance of BIPM was found to be the sum of the dialysate flow rate (QD) and filtrate flow rate (QF). Non-CHDF clearance showed inter-individual variability (4.82 +/- 2.48 L/h), depending on residual renal function and non-renal clearance. Based on the average PK parameters obtained with a compartmental model, maximal kill end point (over 40 % T > MIC4 mug/mL) was achieved with regimens of 300 mg every 6 h, 300 mg every 8 h, and 600 mg every 12 h. Monte Carlo simulation indicated that 300 mg infusion for 1 h every 6 h was optimal, and the probability of target attainment at MIC2 mug/mL was 90.2 %. CONCLUSIONS: Our results establish the optimal regimen of BIPM in patients with various levels of renal function undergoing CHDF with a PS membrane.

Efficacy and safety of biapenem against lower respiratory tract infections in elderly Chinese patients and optimal dosing regimen based on pharmacokinetic/pharmacodynamic analysis.[Pubmed:26430768]

J Chemother. 2016 Oct;28(5):403-10.

The present study evaluated the efficacy and safety of Biapenem in elderly Chinese patients with lower respiratory tract infections (LRTIs) and proposed optimal dosage regimen on the basis of pharmacokinetic/pharmacodynamic (PK/PD) analysis. The clinical efficacy, bacterial eradication and comprehensive therapeutic effect rates of Biapenem were 70.3 (78/111), 68.5 (37/54) and 61.1% (33/54), respectively. Drug-related adverse reactions were seen in 12.6% of patients (14/111). The total protein level, Acute Physiology and Chronic Health Evaluation (APACHE) II score, %fT>MIC, fAUC24/MIC and fCmax/MIC values of patients had significant impacts (P < 0.05) on clinical and bacteriological efficacy. However, logistic regression analysis showed that only %fT>MIC independently influenced comprehensive therapeutic effect (P < 0.01, odds ratio = 1.064). The cut-off value for predicting comprehensive therapeutic effect using %fT>MIC was 75.0%; the sensitivity and specificity were 87.9 and 85.7%, respectively. Monte Carlo simulations revealed that the usual dosage regimen (300 mg every 12 hours, 0.5 hour infusion) was considered to be insufficient to obtain satisfactory therapeutic outcomes against low susceptible pathogens for elderly Chinese patients with LRTIs (CLcr = 70 ml/min).

Clinical effect of biapenem on nursing and healthcare-associated pneumonia (NHCAP).[Pubmed:26050019]

J Infect Chemother. 2015 Aug;21(8):592-5.

The clinical effect of Biapenem (BIPM) on Nursing and Healthcare-associated pneumonia (NHCAP) was evaluated. One hundred and three NHCAP patients (Group B: 52 patients, Group C: 51 patients) to whom BIPM was administered were included in this study. Clinical effect, bacteriological effect, and adverse events were examined. Results revealed efficacy in 45 of 52 patients (efficacy rate: 86.5%) of NHCAP Group B, and 43 of 51 patients (efficacy rate: 84.3%) of NHCAP Group C, 88 of 103 patients (efficacy rate: 85.4%) as a whole. As for bacteriological effect, 10 (76.9%) of 13 Pseudomonas aeruginosa strains, 9 (90.0%) of 10 Klebsiella pneumoniae strains, 7 (87.5%) of 8 methicillin-sensitive Staphlococcus aureus strains, and 7 (100%) of 7 Streptococcus pneumonia strains were eradicated. As a whole, 38 (80.9%) of 47 strains were eradicated. Adverse events included drug fever and drug eruption in one patient each, and abnormal laboratory findings, including mild hepatic dysfunction in 18 patients and mild renal dysfunction in 5 patients. Based on the above, it was concluded that BIPM shows excellent clinical effect on NHCAP with fewer adverse events.

Optimal dosing regimen of biapenem in Chinese patients with lower respiratory tract infections based on population pharmacokinetic/pharmacodynamic modelling and Monte Carlo simulation.[Pubmed:26895604]

Int J Antimicrob Agents. 2016 Mar;47(3):202-9.

In this study, a population pharmacokinetic (PPK) model of Biapenem in Chinese patients with lower respiratory tract infections (LRTIs) was developed and optimal dosage regimens based on Monte Carlo simulation were proposed. A total of 297 plasma samples from 124 Chinese patients were assayed chromatographically in a prospective, single-centre, open-label study, and pharmacokinetic parameters were analysed using NONMEN. Creatinine clearance (CLCr) was found to be the most significant covariate affecting drug clearance. The final PPK model was: CL (L/h)=9.89+(CLCr-66.56)x0.049; Vc (L)=13; Q (L/h)=8.74; and Vp (L)=4.09. Monte Carlo simulation indicated that for a target of >/=40% T>MIC (duration that the plasma level exceeds the causative pathogen's MIC), the Biapenem pharmacokinetic/pharmacodynamic (PK/PD) breakpoint was 4mug/mL for doses of 0.3g every 6h (3-h infusion) and 1.2g (24-h continuous infusion). For a target of >/=80% T>MIC, the PK/PD breakpoint was 4mug/mL for a dose of 1.2g (24-h continuous infusion). The probability of target attainment (PTA) could not achieve >/=90% at the usual Biapenem dosage regimen (0.3g every 12h, 0.5-h infusion) when the MIC of the pathogenic bacteria was 4mug/mL, which most likely resulted in unsatisfactory clinical outcomes in Chinese patients with LRTIs. Higher doses and longer infusion time would be appropriate for empirical therapy. When the patient's symptoms indicated a strong suspicion of Pseudomonas aeruginosa or Acinetobacter baumannii infection, it may be more appropriate for combination therapy with other antibacterial agents.

Description

Biapenem (CLI 86815; L 627; LJC 10627) a parenteral carbapenem antibacterial agent with a broad spectrum.

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