| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Abacavir is present in small amounts in breast milk. Information on the safety of abacavir during lactation is very limited. Achieving and maintaining viral suppression through antiretroviral therapy can reduce the risk of breast milk transmission to below 1%, but not zero. For HIV-infected individuals receiving antiretroviral therapy with a persistently low viral load, breastfeeding should be encouraged if chosen. If viral load is not suppressed, pasteurized donor breast milk or formula is recommended. ◉ Effects on Breastfed Infants An HIV-positive mother took a once-daily combination tablet (Triumeq) containing 50 mg dolutegravir, 600 mg abacavir sulfate, and 300 mg lamivudine. Her infant was exclusively breastfed for approximately 30 weeks, followed by partial breastfeeding for approximately 20 weeks. No significant side effects were observed. ◉ Effects on Lactation and Breast Milk Gynecomastia has been reported in men receiving highly active antiretroviral therapy. Gynecomastia initially presents unilaterally, but approximately half of cases progress to bilateral gynecomastia. No changes in serum prolactin levels were observed, and it usually resolves spontaneously within a year even with continued treatment. Some case reports and in vitro studies suggest that protease inhibitors may cause hyperprolactinemia and galactorrhea in some male patients, but this conclusion remains controversial. The implications of these findings for lactating women are unclear. Prolactin levels in established lactating mothers may not affect their ability to breastfeed. |
|---|---|
| References | |
| Additional Infomation |
Epzicom is a fixed-dose combination therapy consisting of abacavir sulfate (a nucleoside reverse transcriptase inhibitor, NRTI, a guanosine analog) and lamivudine (an NRTI, a cytidine analog) for the treatment of human immunodeficiency virus (HIV) infection. After oral administration, abacavir and lamivudine are phosphorylated into active metabolites that competitively incorporate into viral DNA. These metabolites competitively inhibit HIV reverse transcriptase (RT) and act as chain terminators in DNA synthesis. This interferes with the generation of viral RNA DNA copies, which are essential for the synthesis of new viral particles.
|
| Molecular Formula |
C14H18N6O
|
|---|---|
| Molecular Weight |
286.33
|
| Exact Mass |
286.154
|
| CAS # |
136470-79-6
|
| Related CAS # |
Abacavir;136470-78-5;Abacavir sulfate;188062-50-2;Abacavir monosulfate;216699-07-9;Abacavir hydrochloride;136777-48-5
|
| PubChem CID |
469584
|
| Appearance |
Typically exists as solids at room temperature
|
| LogP |
1.095
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
21
|
| Complexity |
414
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
c1nc2c(nc(nc2n1[C@H]3C[C@H](C=C3)CO)N)NC4CC4CopyCopied
|
| InChi Key |
MCGSCOLBFJQGHM-WCBMZHEXSA-N
|
| InChi Code |
InChI=1S/C14H18N6O/c15-14-18-12(17-9-2-3-9)11-13(19-14)20(7-16-11)10-4-1-8(5-10)6-21/h1,4,7-10,21H,2-3,5-6H2,(H3,15,17,18,19)/t8-,10+/m0/s1
|
| Chemical Name |
[(1R,4S)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methanol
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4925 mL | 17.4624 mL | 34.9247 mL | |
| 5 mM | 0.6985 mL | 3.4925 mL | 6.9849 mL | |
| 10 mM | 0.3492 mL | 1.7462 mL | 3.4925 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.
Link: https://clinicaltrials.gov/ct2/show/NCT02470650
Conditions:Patient Compliance|Antiretroviral Therapy IntoleranceLink: https://clinicaltrials.gov/ct2/show/NCT04493216
Conditions:HIV InfectionsLink: https://clinicaltrials.gov/ct2/show/NCT02120352
Conditions:Infection, Human Immunodeficiency Virus|HIV Infections
Title:Cellular Pharmacology and Platelet Effects of Abacavir and Lamivudine Anabolites
Status:Completed
updateDate:2023-01-09
Ctid:NCT04301661
Link: https://clinicaltrials.gov/ct2/show/NCT04301661
Conditions:HIV-1-infectionLink: https://clinicaltrials.gov/ct2/show/NCT01352715
Conditions:HIV-1 InfectionLink: https://clinicaltrials.gov/ct2/show/NCT02603107
Conditions:HIV-1 InfectionLink: https://clinicaltrials.gov/ct2/show/NCT00044577
Conditions:Infection, Human Immunodeficiency Virus I|HIV InfectionLink: https://clinicaltrials.gov/ct2/show/NCT00046176
Conditions:Infection, Human Immunodeficiency Virus I|HIV InfectionLink: https://clinicaltrials.gov/ct2/show/NCT02469246
Conditions:HIV-1 InfectionLink: https://clinicaltrials.gov/ct2/show/NCT01900106
Conditions:HIV InfectionLink: https://clinicaltrials.gov/ct2/show/NCT02605954
Conditions:HIV-1 InfectionLink: https://clinicaltrials.gov/ct2/show/NCT00118898
Conditions:HIV InfectionsLink: https://clinicaltrials.gov/ct2/show/NCT01263015
Conditions:Infection, Human Immunodeficiency Virus ILink: https://clinicaltrials.gov/ct2/show/NCT02246998
Conditions:HIV-1 InfectionLink: https://clinicaltrials.gov/ct2/show/NCT02893488
Conditions:Infection, Human Immunodeficiency VirusLink: https://clinicaltrials.gov/ct2/show/NCT01608269
Conditions:HiV1- PositiveLink: https://clinicaltrials.gov/ct2/show/NCT01102972
Conditions:Infection, Human Immunodeficiency VirusLink: https://clinicaltrials.gov/ct2/show/NCT00865007
Conditions:HIV Infection|Lipodystrophy|HIV InfectionsLink: https://clinicaltrials.gov/ct2/show/NCT00085943
Conditions:HIV Infection|Infection, Human Immunodeficiency VirusLink: https://clinicaltrials.gov/ct2/show/NCT01220232
Conditions:Healthy VolunteersLink: https://clinicaltrials.gov/ct2/show/NCT00053638
Conditions:HIV InfectionLink: https://clinicaltrials.gov/ct2/show/NCT00094367
Conditions:HIV InfectionLink: https://clinicaltrials.gov/ct2/show/NCT00244712
Conditions:HIV InfectionProducts are for research use only; We do not sell to patients
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