Details
Stereochemistry | RACEMIC |
Molecular Formula | C8H11N3O3S |
Molecular Weight | 229.256 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=NC(=O)N(C=C1)[C@@H]2CS[C@@H](CO)O2
InChI
InChIKey=JTEGQNOMFQHVDC-BQBZGAKWSA-N
InChI=1S/C8H11N3O3S/c9-5-1-2-11(8(13)10-5)6-4-15-7(3-12)14-6/h1-2,6-7,12H,3-4H2,(H2,9,10,13)/t6-,7-/m0/s1
Molecular Formula | C8H11N3O3S |
Molecular Weight | 229.256 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020564s035,020596s034lbl.pdfhttps://pharmaffiliates.com/%C2%B1-trans-lamivudine/lamivudine-impurity-b-impurity/62787 | https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020564s035,020596s034lbl.pdf | https://newdrugapprovals.org/2016/03/18/lamivudine/Curator's Comment: Description was created based on several sources, including:
http://www.drugbank.ca/drugs/DB00709
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2df7349c-f5d7-47b5-d29b-1b6b31985591
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020564s035,020596s034lbl.pdfhttps://pharmaffiliates.com/%C2%B1-trans-lamivudine/lamivudine-impurity-b-impurity/62787 | https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020564s035,020596s034lbl.pdf | https://newdrugapprovals.org/2016/03/18/lamivudine/
Curator's Comment: Description was created based on several sources, including:
http://www.drugbank.ca/drugs/DB00709
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2df7349c-f5d7-47b5-d29b-1b6b31985591
Lamivudine is a reverse transcriptase inhibitor used alone or in combination with other classes of anti-human immunodeficiency virus (HIV) drugs in the treatment of HIV infection. This molecule has two stereo-centers, thus giving rise to four stereoisomers: (+/-)-cis-lamivudine and (+/-)-trans-lamivudine. The latter is considered to be impurity of the pharmaceutically active isomer, (-)-cis-lamivudine.
CNS Activity
Sources: http://www.ncbi.nlm.nih.gov/pubmed/22514580
Curator's Comment: Known to be CNS penetrant in rat, guinea pig. Human data not available.
http://www.ncbi.nlm.nih.gov/pubmed/9593963
http://www.ncbi.nlm.nih.gov/pubmed/18042828
http://www.ncbi.nlm.nih.gov/pubmed/12766261
Originator
Sources: http://www.thepharmaletter.com/article/lamivudine-positive-effects-in-hepatitis-bhttps://www.ncbi.nlm.nih.gov/pubmed/1929298
Curator's Comment: http://www.google.com/patents/US20030004175?hl=ru&cl=en
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL247 |
2.0 nM [IC50] | ||
Target ID: CHEMBL2362994 |
3.3 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | EPIVIR Approved UseEPIVIR is a nucleoside analogue indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection. Launch Date2004 |
|||
Primary | EPIVIR Approved UseEPIVIR-HBV is a nucleoside analogue reverse transcriptase inhibitor indicated for the treatment of chronic hepatitis B virus infection associated with evidence of hepatitis B viral replication and active liver inflammation Launch Date2004 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.3 μg/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29150845 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
LAMIVUDINE blood | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1.4 μg/mL |
150 mg 2 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LAMIVUDINE unknown | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
12.4 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29150845 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
LAMIVUDINE blood | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
5.53 μg × h/mL |
150 mg 2 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
LAMIVUDINE unknown | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
13.9 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29150845 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
LAMIVUDINE blood | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 14.6 n = 12 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 14.6 Sex: M+F Population Size: 12 Sources: |
Other AEs: Malaise and fatigue, Ear, nose and throat infection... Other AEs: Malaise and fatigue (25%) Sources: Ear, nose and throat infection (17%) Cough (8%) Headache (17%) Nausea and vomiting (8%) Ear, nose and throat infection (8%) |
10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Other AEs: Coughing, Diarrhea... Other AEs: Coughing (6 patients) Sources: Diarrhea (9 patients) Abdominal discomfort (2 patients) Nausea and vomiting (1 patient) Malaise and fatigue (6 patients) Headache (6 patients) Disorder sleep (4 patients) Cognitive disorders (2 patients) Oral ulceration (2 patients) Oral lesion (2 patients) Muscle pain (3 patients) Arthralgia (1 patient) Temperature regulation disorder (2 patients) |
4 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 4 mg/kg, 2 times / day Route: oral Route: multiple Dose: 4 mg/kg, 2 times / day Sources: |
unhealthy, 7.6 n = 11 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 7.6 Sex: M+F Population Size: 11 Sources: |
Other AEs: Malaise and fatigue, Cough... Other AEs: Malaise and fatigue (27%) Sources: Cough (27%) Temperature regulation disorder NOS (27%) Nausea and vomiting (9%) Ear, nose and throat infection (18%) Ear disorder (9%) Pharyngitis (18%) |
150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Other AEs: Headache, Malaise and fatigue... Other AEs: Headache (35%) Sources: Malaise and fatigue (27%) Chills & fever (10%) Nausea (33%) Diarrhea (18%) Nausea and vomiting (13%) Decreased appetite (10%) Abdominal pain (9%) Abdominal cramps (6%) Dyspepsia (5%) Neuropathy (12%) Insomnia disorder (11%) Dizziness (10%) Depressive disorders (9%) Nasal disorders NEC (20%) Cough (18%) Skin rash (9%) Musculoskeletal pain (12%) Myalgia (8%) Arthralgia (5%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Ear, nose and throat infection | 17% | 100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 14.6 n = 12 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 14.6 Sex: M+F Population Size: 12 Sources: |
Headache | 17% | 100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 14.6 n = 12 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 14.6 Sex: M+F Population Size: 12 Sources: |
Malaise and fatigue | 25% | 100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 14.6 n = 12 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 14.6 Sex: M+F Population Size: 12 Sources: |
Cough | 8% | 100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 14.6 n = 12 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 14.6 Sex: M+F Population Size: 12 Sources: |
Ear, nose and throat infection | 8% | 100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 14.6 n = 12 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 14.6 Sex: M+F Population Size: 12 Sources: |
Nausea and vomiting | 8% | 100 mg 1 times / day multiple, oral Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 14.6 n = 12 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 14.6 Sex: M+F Population Size: 12 Sources: |
Arthralgia | 1 patient | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Nausea and vomiting | 1 patient | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Abdominal discomfort | 2 patients | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Cognitive disorders | 2 patients | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Oral lesion | 2 patients | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Oral ulceration | 2 patients | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Temperature regulation disorder | 2 patients | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Muscle pain | 3 patients | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Disorder sleep | 4 patients | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Coughing | 6 patients | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Headache | 6 patients | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Malaise and fatigue | 6 patients | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Diarrhea | 9 patients | 10 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 10 mg/kg, 2 times / day Route: oral Route: multiple Dose: 10 mg/kg, 2 times / day Sources: |
unhealthy, 37 years (range: 23-63 years) n = 14 Health Status: unhealthy Condition: HIV infection Age Group: 37 years (range: 23-63 years) Population Size: 14 Sources: |
Ear, nose and throat infection | 18% | 4 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 4 mg/kg, 2 times / day Route: oral Route: multiple Dose: 4 mg/kg, 2 times / day Sources: |
unhealthy, 7.6 n = 11 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 7.6 Sex: M+F Population Size: 11 Sources: |
Pharyngitis | 18% | 4 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 4 mg/kg, 2 times / day Route: oral Route: multiple Dose: 4 mg/kg, 2 times / day Sources: |
unhealthy, 7.6 n = 11 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 7.6 Sex: M+F Population Size: 11 Sources: |
Cough | 27% | 4 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 4 mg/kg, 2 times / day Route: oral Route: multiple Dose: 4 mg/kg, 2 times / day Sources: |
unhealthy, 7.6 n = 11 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 7.6 Sex: M+F Population Size: 11 Sources: |
Malaise and fatigue | 27% | 4 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 4 mg/kg, 2 times / day Route: oral Route: multiple Dose: 4 mg/kg, 2 times / day Sources: |
unhealthy, 7.6 n = 11 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 7.6 Sex: M+F Population Size: 11 Sources: |
Temperature regulation disorder NOS | 27% | 4 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 4 mg/kg, 2 times / day Route: oral Route: multiple Dose: 4 mg/kg, 2 times / day Sources: |
unhealthy, 7.6 n = 11 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 7.6 Sex: M+F Population Size: 11 Sources: |
Ear disorder | 9% | 4 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 4 mg/kg, 2 times / day Route: oral Route: multiple Dose: 4 mg/kg, 2 times / day Sources: |
unhealthy, 7.6 n = 11 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 7.6 Sex: M+F Population Size: 11 Sources: |
Nausea and vomiting | 9% | 4 mg/kg 2 times / day multiple, oral Highest studied dose Dose: 4 mg/kg, 2 times / day Route: oral Route: multiple Dose: 4 mg/kg, 2 times / day Sources: |
unhealthy, 7.6 n = 11 Health Status: unhealthy Condition: Chronic hepatitis B Age Group: 7.6 Sex: M+F Population Size: 11 Sources: |
Chills & fever | 10% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Decreased appetite | 10% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Dizziness | 10% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Insomnia disorder | 11% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Musculoskeletal pain | 12% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Neuropathy | 12% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Nausea and vomiting | 13% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Cough | 18% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Diarrhea | 18% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Nasal disorders NEC | 20% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Malaise and fatigue | 27% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Nausea | 33% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Headache | 35% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Arthralgia | 5% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Dyspepsia | 5% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Abdominal cramps | 6% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Myalgia | 8% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Abdominal pain | 9% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Depressive disorders | 9% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Skin rash | 9% | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Co-administed with:: zidovudine(200 mg; 3/day) Sources: |
unhealthy n = 251 Health Status: unhealthy Condition: HIV-1 infection Population Size: 251 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
Sources: https://www.pmda.go.jp/drugs/2020/P20200109001/340278000_30200AMX00001_I100_1.pdf#page=6 Page: 6.0 |
no | |||
Sources: https://www.pmda.go.jp/drugs/2020/P20200109001/340278000_30200AMX00001_I100_1.pdf#page=6 Page: 6.0 |
no | |||
Sources: https://www.pmda.go.jp/drugs/2020/P20200109001/340278000_30200AMX00001_I100_1.pdf#page=6 Page: 6.0 |
no | |||
weak to no | ||||
weak to no | ||||
weak to no | ||||
Sources: https://www.pmda.go.jp/drugs/2020/P20200109001/340278000_30200AMX00001_I100_1.pdf#page=6 Page: 6.0 |
yes | |||
Sources: https://www.pmda.go.jp/drugs/2020/P20200109001/340278000_30200AMX00001_I100_1.pdf#page=6 Page: 6.0 |
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
not signifiicant | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020564s039,020596s038lbl.pdf#page=19 Page: 19.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020564s039,020596s038lbl.pdf#page=19 Page: 19.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020564s039,020596s038lbl.pdf#page=19 Page: 19.0 |
yes | |||
yes | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020564s039,020596s038lbl.pdf#page=19 Page: 19.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020564s039,020596s038lbl.pdf#page=19 Page: 19.0 |
yes |
PubMed
Title | Date | PubMed |
---|---|---|
A novel genotype encoding a single amino acid insertion and five other substitutions between residues 64 and 74 of the HIV-1 reverse transcriptase confers high-level cross-resistance to nucleoside reverse transcriptase inhibitors. Abacavir CNA2007 International Study Group. | 1999 Oct 1 |
|
Antiviral combination therapy for lamivudine-resistant hepatitis B reinfection after liver transplantation. | 2000 |
|
Long-term exposure of HIV type 1-infected cell cultures to combinations of the novel quinoxaline GW420867X with lamivudine, abacavir, and a variety of nonnucleoside reverse transcriptase inhibitors. | 2000 Apr 10 |
|
Additional interferon alpha for lamivudine resistant hepatitis B infection after liver transplantation: a preliminary report. | 2000 Apr 27 |
|
Small molecule inhibitor of HIV-1 nuclear import suppresses HIV-1 replication in human lymphoid tissue ex vivo: a potential addition to current anti-HIV drug repertoire. | 2000 Aug |
|
Beneficial effects of lamivudine in hepatitis B virus-related decompensated cirrhosis. | 2000 Aug |
|
Inhibitory effect of human immunodeficiency virus protease inhibitors on multidrug resistance transporter P-glycoproteins. | 2000 Dec |
|
Increasing cerebrospinal fluid chemokine concentrations despite undetectable cerebrospinal fluid HIV RNA in HIV-1-infected patients receiving antiretroviral therapy. | 2000 Dec 15 |
|
Long-term follow-up of patients with anti-HBe/HBV DNA-positive chronic hepatitis B treated for 12 months with lamivudine. | 2000 Feb |
|
Lamivudine, adefovir and tenofovir exhibit long-lasting anti-hepatitis B virus activity in cell culture. | 2000 Jan |
|
A randomized, comparative study of lamivudine plus stavudine, with indinavir or nelfinavir, in treatment-experienced HIV-infected patients. | 2000 Jan 28 |
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Differential transport of cytosine-containing nucleosides by recombinant human concentrative nucleoside transporter protein hCNT1. | 2000 Jan-Feb |
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Potentiation of the anti-HIV activity of zalcitabine and lamivudine by a CTP synthase inhibitor, 3-deazauridine. | 2000 Jan-Feb |
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Lamivudine after hepatitis B immune globulin is effective in preventing hepatitis B recurrence after liver transplantation. | 2000 Jul |
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Combination low-dose hepatitis B immune globulin and lamivudine therapy provides effective prophylaxis against posttransplantation hepatitis B. | 2000 Jul |
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Management of hepatitis B in China. | 2000 Jul |
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In vitro selection of mutations in the human immunodeficiency virus type 1 reverse transcriptase that decrease susceptibility to (-)-beta-D-dioxolane-guanosine and suppress resistance to 3'-azido-3'-deoxythymidine. | 2000 Jul |
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Steatosis-lactic acidosis syndrome associated with stavudine and lamivudine therapy. | 2000 Jun 16 |
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Synthesis and antiviral evaluation of some beta-L-2', 3'-dideoxy-5-chloropyrimidine nucleosides and pronucleotides. | 2000 Mar |
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Severe hypertension and renal atrophy associated with indinavir. | 2000 Mar |
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Selection and characterization of human immunodeficiency virus type 1 variants resistant to the (+) and (-) enantiomers of 2'-deoxy-3'-oxa-4'-thio-5-fluorocytidine. | 2000 May |
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Selection of resistance-conferring mutations in HIV-1 by the nucleoside reverse transcriptase inhibitors (+/-)dOTC and (+/-)dOTFC. | 2000 Nov |
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Correlation between intracellular pharmacological activation of nucleoside analogues and HIV suppression in vitro. | 2000 Nov |
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An efficacy and cost-effectiveness analysis of combination hepatitis B immune globulin and lamivudine to prevent recurrent hepatitis B after orthotopic liver transplantation compared with hepatitis B immune globulin monotherapy. | 2000 Nov |
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Clinical improvement in patients with decompensated liver disease caused by hepatitis B after treatment with lamivudine. | 2000 Nov |
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Leucocytoclastic vasculitis and indinavir. | 2000 Nov |
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Successful orthotopic liver transplantation for lamivudine-associated YMDD mutant hepatitis B virus. | 2000 Nov |
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Synthesis and antiviral activity of oxaselenolane nucleosides. | 2000 Oct 19 |
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Sudden unexpected death as a consequence of indinavir-induced nephropathy. A case report. | 2000 Sep |
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Acute exacerbation of chronic hepatitis B virus infection after withdrawal of lamivudine therapy. | 2000 Sep |
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Antiviral beta-L-nucleosides specific for hepatitis B virus infection. | 2001 |
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Anti-HBV specific beta-L-2'-deoxynucleosides. | 2001 Apr-Jul |
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Acyclic/carbocyclic guanosine analogues as anti-herpesvirus agents. | 2001 Apr-Jul |
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Antiviral activity of tenofovir (PMPA) against nucleoside-resistant clinical HIV samples. | 2001 Apr-Jul |
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Successful lamivudine therapy for post-chemotherapeutic fulminant hepatitis B in a hepatitis B virus carrier with non-Hodgkin's lymphoma: case report and review of the literature. | 2001 Aug |
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Prenatal AZT or 3TC and mouse development of locomotor activity and hot-plate responding upon administration of the GABA(A) receptor agonist muscimol. | 2001 Feb |
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Interferon therapy for flare-up of hepatitis B virus infection after emergence of lamivudine-induced YMDD motif mutant. | 2001 Feb |
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Liver transplantation in Asian patients with chronic hepatitis B using lamivudine prophylaxis. | 2001 Feb |
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A multicenter United States-Canadian trial to assess lamivudine monotherapy before and after liver transplantation for chronic hepatitis B. | 2001 Feb |
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Antiviral L-nucleosides specific for hepatitis B virus infection. | 2001 Jan |
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[Treatment of chronic viral hepatitis B with lamivudine]. | 2001 Jan 27 |
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Nelfinavir in expanded postexposure prophylaxis causing acute hepatitis with cholestatic features: two case reports. | 2001 Jun |
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A multicenter study of lamivudine treatment in 33 patients with hepatitis B after liver transplantation. | 2001 Jun |
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Updated U.S. Public Health Service Guidelines for the Management of Occupational Exposures to HBV, HCV, and HIV and Recommendations for Postexposure Prophylaxis. | 2001 Jun 29 |
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The real danger of lamivudine-resistant hepatitis B virus infection in the immunocompromised host. | 2001 Mar |
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Efavirenz-induced acute eosinophilic hepatitis. | 2001 May |
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Differential human immunodeficiency virus-suppressive activity of reverse transcription inhibitors in resting and activated peripheral blood lymphocytes: implications for therapy. | 2001 May-Jun |
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Novel 5-vinyl pyrimidine nucleosides with potent anti-hepatitis B virus activity. | 2001 Nov 19 |
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Lamivudine treatment for hepatitis B reactivation in HBsAg carriers after organ transplantation: a 4-year experience. | 2001 Sep |
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Specific inhibition of human immunodeficiency virus type 1 (HIV-1) integration in cell culture: putative inhibitors of HIV-1 integrase. | 2001 Sep |
Patents
Sample Use Guides
In Vivo Use Guide
Curator's Comment: Pediatric dose should be calculated on body weight (kg) and should not exceed 300 mg daily.
Dosage of this product is for HIV-1 and not for HBV
Adults: 300 mg daily, administered as either 150 mg twice daily or 300 mg once daily.
Route of Administration:
Oral
The antiviral activity of lamivudine against HIV-1 was assessed in a number of cell lines including monocytes and fresh human peripheral blood lymphocytes (PBMCs) using standard susceptibility assays. EC50 values were in the range of 0.003 to 15 microM (1 microM = 0.23 mcg per mL).
Substance Class |
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