Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C47H73NO17.C24H39O4.Na |
Molecular Weight | 1338.6328 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 29 / 29 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].[H][C@@]1(CC[C@@]2([H])[C@]3([H])CC[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])C[C@H](O)[C@]12C)[C@H](C)CCC([O-])=O.[H][C@]56C[C@@H](O[C@@H]7O[C@H](C)[C@@H](O)[C@H](N)[C@@H]7O)\C=C\C=C\C=C\C=C\C=C\C=C\C=C\[C@H](C)[C@@H](O)[C@@H](C)[C@H](C)OC(=O)C[C@H](O)C[C@H](O)CC[C@@H](O)[C@H](O)C[C@H](O)C[C@](O)(C[C@H](O)[C@H]5C(O)=O)O6
InChI
InChIKey=NFHDUMMQBQTVTR-OXEBIIQQSA-M
InChI=1S/C47H73NO17.C24H40O4.Na/c1-27-17-15-13-11-9-7-5-6-8-10-12-14-16-18-34(64-46-44(58)41(48)43(57)30(4)63-46)24-38-40(45(59)60)37(54)26-47(61,65-38)25-33(51)22-36(53)35(52)20-19-31(49)21-32(50)23-39(55)62-29(3)28(2)42(27)56;1-14(4-9-22(27)28)18-7-8-19-17-6-5-15-12-16(25)10-11-23(15,2)20(17)13-21(26)24(18,19)3;/h5-18,27-38,40-44,46,49-54,56-58,61H,19-26,48H2,1-4H3,(H,59,60);14-21,25-26H,4-13H2,1-3H3,(H,27,28);/q;;+1/p-1/b6-5+,9-7+,10-8+,13-11+,14-12+,17-15+,18-16+;;/t27-,28-,29-,30+,31+,32+,33-,34-,35+,36+,37-,38-,40+,41-,42+,43+,44-,46-,47+;14-,15-,16-,17+,18-,19+,20+,21+,23+,24-;/m01./s1
Molecular Formula | C24H39O4 |
Molecular Weight | 391.5641 |
Charge | -1 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 10 / 10 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Molecular Formula | Na |
Molecular Weight | 22.9898 |
Charge | 1 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C47H73NO17 |
Molecular Weight | 924.079 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 19 / 19 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.x-gen.us/wp-content/uploads/sites/21/2014/03/XGSS_TSM_AMPH.03.15.pdfhttps://www.ncbi.nlm.nih.gov/pubmed/22869574Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/24366747 | https://www.aceabiotech.com/corifungin/ | https://www.aceabiotech.com/clinical-development-of-corifungin/ | https://www.google.com/patents/US20130123205 | https://www.ncbi.nlm.nih.gov/pubmed/26259797
Sources: http://www.x-gen.us/wp-content/uploads/sites/21/2014/03/XGSS_TSM_AMPH.03.15.pdfhttps://www.ncbi.nlm.nih.gov/pubmed/22869574
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/24366747 | https://www.aceabiotech.com/corifungin/ | https://www.aceabiotech.com/clinical-development-of-corifungin/ | https://www.google.com/patents/US20130123205 | https://www.ncbi.nlm.nih.gov/pubmed/26259797
Corifungin refers to the sodium salt of amphotericin B. Although amphotericin B has become the primary drug of choice for treating primary amoebic meningoencephalitis, its use is associated with multiple side effects, including use-limiting renal toxicity. Initial reports for the in vivo efficacy of corifungin in a mouse model of primary amoebic meningoencephalitis showed activity superior to that of amphotericin B at equivalent dosing. Chemically, corifungin is the sodium salt of amphotericin B with excellent aqueous solubility. The increased solubility of corifungin is likely to account for the described increase in activity. Acea Biotech is developing corifungin for the treatment of fungal infections and amebic diseases. Acea has completed of host of animal studies on corifungin setting the stage to take the drug into the clinic. U.S. FDA has approved orphan drug status for corifungin for the treatment of primary amebic meningoencephalitis.
CNS Activity
Sources: https://www.medicine.wisc.edu/sites/default/files/domfiles/infectiousdisease/EMT030408.pdfhttps://www.ncbi.nlm.nih.gov/pubmed/24366747 | https://www.ncbi.nlm.nih.gov/pubmed/22869574
Curator's Comment: The absence of detectable amebae in the brain of a corifungin-treated mouse model of primary amebic meningoencephalitis was demonstrated. This suggests that corifungin may have the ability to cross the blood-brain barrier because of enhanced solubility although this has not been tested.
Originator
Sources: https://patents.google.com/patent/US2908611A/enhttp://adisinsight.springer.com/drugs/800030928 | https://www.google.com/patents/US20130123205
Curator's Comment: Amphotericin B was originally extracted from Streptomyces nodosus in 1955 at the Squibb Institute for Medical Research. The first synthesis of the Amphotericin B was achieved in 1988 at the University of Pennsylvania. Today X-gen Pharms (formerly Pharma Tek) develop conventional Amphotericin B for Injection (approved since 1992).
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2364028 Sources: http://www.ncbi.nlm.nih.gov/pubmed/19689243 |
|||
Target ID: GO:0071555 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Curative | Unknown Approved UseUnknown |
|||
Curative | Unknown Approved UseUnknown |
|||
Curative | AMPHOTERICIN B Approved UseAmphotericin B for Injection USP should be administered primarily to patients with progressive, potentially life-threatening fungal infections. This potent drug should not be used to treat noninvasive fungal infections, such as oral thrush, vaginal candidiasis and esophageal candidiasis in patients with normal neutrophil counts.
Amphotericin B for Injection USP is specifically intended to treat potentially life-threatening fungal infections: aspergillosis, cryptococcosis (torulosis), North American blastomycosis, systemic candidiasis, coccidioido-mycosis, histoplasmosis, zygomycosis including mucormycosis due to
susceptible species of the genera Absidia, Mucor and Rhizopus, and infections due to related susceptible species of Conidiobolus and Basidiobolus, and sporotrichosis.
Amphotericin B may be useful in the treatment of American mucocutaneous leishmaniasis, but it is not the drug of choice as primary therapy. Launch Date1992 |
|||
Curative | AMPHOTERICIN B Approved UseAmphotericin B for Injection USP should be administered primarily to patients with progressive, potentially life-threatening fungal infections. This potent drug should not be used to treat noninvasive fungal infections, such as oral thrush, vaginal candidiasis and esophageal candidiasis in patients with normal neutrophil counts.
Amphotericin B for Injection USP is specifically intended to treat potentially life-threatening fungal infections: aspergillosis, cryptococcosis (torulosis), North American blastomycosis, systemic candidiasis, coccidioido-mycosis, histoplasmosis, zygomycosis including mucormycosis due to
susceptible species of the genera Absidia, Mucor and Rhizopus, and infections due to related susceptible species of Conidiobolus and Basidiobolus, and sporotrichosis.
Amphotericin B may be useful in the treatment of American mucocutaneous leishmaniasis, but it is not the drug of choice as primary therapy. Launch Date1992 |
|||
Curative | AMPHOTERICIN B Approved UseAmphotericin B for Injection USP should be administered primarily to patients with progressive, potentially life-threatening fungal infections. This potent drug should not be used to treat noninvasive fungal infections, such as oral thrush, vaginal candidiasis and esophageal candidiasis in patients with normal neutrophil counts.
Amphotericin B for Injection USP is specifically intended to treat potentially life-threatening fungal infections: aspergillosis, cryptococcosis (torulosis), North American blastomycosis, systemic candidiasis, coccidioido-mycosis, histoplasmosis, zygomycosis including mucormycosis due to
susceptible species of the genera Absidia, Mucor and Rhizopus, and infections due to related susceptible species of Conidiobolus and Basidiobolus, and sporotrichosis.
Amphotericin B may be useful in the treatment of American mucocutaneous leishmaniasis, but it is not the drug of choice as primary therapy. Launch Date1992 |
|||
Curative | AMPHOTERICIN B Approved UseAmphotericin B for Injection USP should be administered primarily to patients with progressive, potentially life-threatening fungal infections. This potent drug should not be used to treat noninvasive fungal infections, such as oral thrush, vaginal candidiasis and esophageal candidiasis in patients with normal neutrophil counts.
Amphotericin B for Injection USP is specifically intended to treat potentially life-threatening fungal infections: aspergillosis, cryptococcosis (torulosis), North American blastomycosis, systemic candidiasis, coccidioido-mycosis, histoplasmosis, zygomycosis including mucormycosis due to
susceptible species of the genera Absidia, Mucor and Rhizopus, and infections due to related susceptible species of Conidiobolus and Basidiobolus, and sporotrichosis.
Amphotericin B may be useful in the treatment of American mucocutaneous leishmaniasis, but it is not the drug of choice as primary therapy. Launch Date1992 |
|||
Curative | AMPHOTERICIN B Approved UseAmphotericin B for Injection USP should be administered primarily to patients with progressive, potentially life-threatening fungal infections. This potent drug should not be used to treat noninvasive fungal infections, such as oral thrush, vaginal candidiasis and esophageal candidiasis in patients with normal neutrophil counts.
Amphotericin B for Injection USP is specifically intended to treat potentially life-threatening fungal infections: aspergillosis, cryptococcosis (torulosis), North American blastomycosis, systemic candidiasis, coccidioido-mycosis, histoplasmosis, zygomycosis including mucormycosis due to
susceptible species of the genera Absidia, Mucor and Rhizopus, and infections due to related susceptible species of Conidiobolus and Basidiobolus, and sporotrichosis.
Amphotericin B may be useful in the treatment of American mucocutaneous leishmaniasis, but it is not the drug of choice as primary therapy. Launch Date1992 |
|||
Curative | AMPHOTERICIN B Approved UseAmphotericin B for Injection USP should be administered primarily to patients with progressive, potentially life-threatening fungal infections. This potent drug should not be used to treat noninvasive fungal infections, such as oral thrush, vaginal candidiasis and esophageal candidiasis in patients with normal neutrophil counts.
Amphotericin B for Injection USP is specifically intended to treat potentially life-threatening fungal infections: aspergillosis, cryptococcosis (torulosis), North American blastomycosis, systemic candidiasis, coccidioido-mycosis, histoplasmosis, zygomycosis including mucormycosis due to
susceptible species of the genera Absidia, Mucor and Rhizopus, and infections due to related susceptible species of Conidiobolus and Basidiobolus, and sporotrichosis.
Amphotericin B may be useful in the treatment of American mucocutaneous leishmaniasis, but it is not the drug of choice as primary therapy. Launch Date1992 |
|||
Curative | AMPHOTERICIN B Approved UseAmphotericin B for Injection USP should be administered primarily to patients with progressive, potentially life-threatening fungal infections. This potent drug should not be used to treat noninvasive fungal infections, such as oral thrush, vaginal candidiasis and esophageal candidiasis in patients with normal neutrophil counts.
Amphotericin B for Injection USP is specifically intended to treat potentially life-threatening fungal infections: aspergillosis, cryptococcosis (torulosis), North American blastomycosis, systemic candidiasis, coccidioido-mycosis, histoplasmosis, zygomycosis including mucormycosis due to
susceptible species of the genera Absidia, Mucor and Rhizopus, and infections due to related susceptible species of Conidiobolus and Basidiobolus, and sporotrichosis.
Amphotericin B may be useful in the treatment of American mucocutaneous leishmaniasis, but it is not the drug of choice as primary therapy. Launch Date1992 |
|||
Curative | AMPHOTERICIN B Approved UseAmphotericin B for Injection USP should be administered primarily to patients with progressive, potentially life-threatening fungal infections. This potent drug should not be used to treat noninvasive fungal infections, such as oral thrush, vaginal candidiasis and esophageal candidiasis in patients with normal neutrophil counts.
Amphotericin B for Injection USP is specifically intended to treat potentially life-threatening fungal infections: aspergillosis, cryptococcosis (torulosis), North American blastomycosis, systemic candidiasis, coccidioido-mycosis, histoplasmosis, zygomycosis including mucormycosis due to
susceptible species of the genera Absidia, Mucor and Rhizopus, and infections due to related susceptible species of Conidiobolus and Basidiobolus, and sporotrichosis.
Amphotericin B may be useful in the treatment of American mucocutaneous leishmaniasis, but it is not the drug of choice as primary therapy. Launch Date1992 |
|||
Curative | AMPHOTERICIN B Approved UseAmphotericin B for Injection USP should be administered primarily to patients with progressive, potentially life-threatening fungal infections. This potent drug should not be used to treat noninvasive fungal infections, such as oral thrush, vaginal candidiasis and esophageal candidiasis in patients with normal neutrophil counts.
Amphotericin B for Injection USP is specifically intended to treat potentially life-threatening fungal infections: aspergillosis, cryptococcosis (torulosis), North American blastomycosis, systemic candidiasis, coccidioido-mycosis, histoplasmosis, zygomycosis including mucormycosis due to
susceptible species of the genera Absidia, Mucor and Rhizopus, and infections due to related susceptible species of Conidiobolus and Basidiobolus, and sporotrichosis.
Amphotericin B may be useful in the treatment of American mucocutaneous leishmaniasis, but it is not the drug of choice as primary therapy. Launch Date1992 |
|||
Curative | AMPHOTERICIN B Approved UseAmphotericin B for Injection USP should be administered primarily to patients with progressive, potentially life-threatening fungal infections. This potent drug should not be used to treat noninvasive fungal infections, such as oral thrush, vaginal candidiasis and esophageal candidiasis in patients with normal neutrophil counts.
Amphotericin B for Injection USP is specifically intended to treat potentially life-threatening fungal infections: aspergillosis, cryptococcosis (torulosis), North American blastomycosis, systemic candidiasis, coccidioido-mycosis, histoplasmosis, zygomycosis including mucormycosis due to
susceptible species of the genera Absidia, Mucor and Rhizopus, and infections due to related susceptible species of Conidiobolus and Basidiobolus, and sporotrichosis.
Amphotericin B may be useful in the treatment of American mucocutaneous leishmaniasis, but it is not the drug of choice as primary therapy. Launch Date1992 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
31.4 μg/mL |
2.5 mg/kg 1 times / day multiple, intravenous dose: 2.5 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
57.6 μg/mL |
5 mg/kg single, intravenous dose: 5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
7.3 μg/mL |
1 mg/kg single, intravenous dose: 1 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
62.4 μg/mL |
7.5 mg/kg 1 times / day multiple, intravenous dose: 7.5 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
83.7 μg/mL |
7.5 mg/kg single, intravenous dose: 7.5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
83 μg/mL |
5 mg/kg 1 times / day multiple, intravenous dose: 5 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
12.2 μg/mL |
1 mg/kg 1 times / day multiple, intravenous dose: 1 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
17.2 μg/mL |
2.5 mg/kg single, intravenous dose: 2.5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
197 μg × h/mL |
2.5 mg/kg 1 times / day multiple, intravenous dose: 2.5 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
269 μg × h/mL |
5 mg/kg single, intravenous dose: 5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
27 μg × h/mL |
1 mg/kg single, intravenous dose: 1 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
382 μg × h/mL |
7.5 mg/kg 1 times / day multiple, intravenous dose: 7.5 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
476 μg × h/mL |
7.5 mg/kg single, intravenous dose: 7.5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
555 μg × h/mL |
5 mg/kg 1 times / day multiple, intravenous dose: 5 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
60 μg × h/mL |
1 mg/kg 1 times / day multiple, intravenous dose: 1 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
65 μg × h/mL |
2.5 mg/kg single, intravenous dose: 2.5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
6.3 h |
2.5 mg/kg 1 times / day multiple, intravenous dose: 2.5 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
6.4 h |
5 mg/kg single, intravenous dose: 5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
10.7 h |
1 mg/kg single, intravenous dose: 1 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
6.9 h |
7.5 mg/kg 1 times / day multiple, intravenous dose: 7.5 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
8.5 h |
7.5 mg/kg single, intravenous dose: 7.5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
6.8 h |
5 mg/kg 1 times / day multiple, intravenous dose: 5 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
7 h |
1 mg/kg 1 times / day multiple, intravenous dose: 1 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
8.1 h |
2.5 mg/kg single, intravenous dose: 2.5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMPHOTERICIN B serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.1% EXPERIMENT https://aac.asm.org/content/46/3/834.long |
AMPHOTERICIN B plasma | Homo sapiens |
Doses
Dose | Population | Adverse events |
---|---|---|
0.7 mg/kg 1 times / day multiple, intravenous Recommended Dose: 0.7 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 0.7 mg/kg, 1 times / day Sources: Page: p. 27 |
unhealthy, 39 years (range: 21-68 years) n = 87 Health Status: unhealthy Age Group: 39 years (range: 21-68 years) Sex: M+F Population Size: 87 Sources: Page: p. 27 |
Disc. AE: Creatinine increased... Other AEs: Nervous system disorder NOS, Cardiovascular injuries... AEs leading to discontinuation/dose reduction: Creatinine increased (3.4%) Other AEs:Nervous system disorder NOS (3.4%) Sources: Page: p. 27Cardiovascular injuries (3.4%) |
5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Other AEs: Thrombocytopenia, Anaemia... Other AEs: Thrombocytopenia (serious, 2 patients) Sources: Anaemia (serious, 1 patient) Neutropenia (serious, 1 patient) Pancytopenia (serious, 1 patient) Cardiac arrest (serious, 4 patients) Cardio-respiratory arrest (serious, 1 patient) Pancreatitis (serious, 2 patients) Ileus (serious, 1 patient) Intestinal obstruction (serious, 1 patient) Upper gastrointestinal haemorrhage (serious, 1 patient) Vomiting (serious, 1 patient) Chills (serious, 1 patient) Mucosal inflammation (serious, 1 patient) Multi-organ failure (serious, 1 patient) Hepatic failure (serious, 2 patients) Bile duct stone (serious, 1 patient) Cholecystitis (serious, 1 patient) Cholecystitis acute (serious, 1 patient) Hepatic steatosis (serious, 1 patient) Hepatocellular injury (serious, 1 patient) Hyperbilirubinaemia (serious, 1 patient) Liver disorder (serious, 1 patient) Drug hypersensitivity (serious, 1 patient) Hypersensitivity (serious, 1 patient) Septic shock (serious, 13 patients) Pneumonia (serious, 7 patients) Device related infection (serious, 3 patients) Clostridium difficile colitis (serious, 1 patient) Enterococcal bacteraemia (serious, 1 patient) Gastroenteritis (serious, 1 patient) Infection staphylococcal (serious, 1 patient) Streptococcal sepsis (serious, 1 patient) Blood creatinine increased (serious, 3 patients) Creatinine renal clearance decreased (serious, 2 patients) Lymphocyte count decreased (serious, 1 patient) White blood cell count decreased (serious, 1 patient) Hypokalaemia (serious, 2 patients) Hyperglycaemia (serious, 1 patient) Hyponatraemia (serious, 1 patient) Back pain (serious, 1 patient) Joint swelling (serious, 1 patient) Metastases to central nervous system (serious, 1 patient) Cerebrovascular accident (serious, 1 patient) Encephalitis (serious, 1 patient) Encephalopathy hepatic (serious, 1 patient) Renal tubular necrosis (serious, 1 patient) Acute respiratory distress syndrome (serious, 2 patients) Bronchospasm (serious, 1 patient) Dyspnoea (serious, 1 patient) Pneumothorax (serious, 1 patient) Respiratory distress (serious, 1 patient) Rash papular (serious, 1 patient) Hypotension (serious, 1 patient) Thrombocytopenia (below serious, 42 patients) Nausea (below serious, 118 patients) Abdominal pain upper (below serious, 39 patients) Dyspepsia (below serious, 14 patients) Oedema peripheral (below serious, 56 patients) Chest pain (below serious, 18 patients) Oedema (below serious, 15 patients) Oral herpes (below serious, 22 patients) Pneumonia (below serious, 15 patients) Aspartate aminotransferase increased (below serious, 19 patients) Blood bilirubin increased (below serious, 16 patients) Blood creatinine increased (below serious, 20 patients) Weight decreased (below serious, 13 patients) Hypokalaemia (below serious, 83 patients) Hypoalbuminaemia (below serious, 24 patients) Hypocalcaemia (below serious, 18 patients) Fluid retention (below serious, 15 patients) Hypomagnesaemia (below serious, 12 patients) Back pain (below serious, 34 patients) Depression (below serious, 12 patients) Rash (below serious, 39 patients) Erythema (below serious, 19 patients) Alopecia (below serious, 17 patients) Pruritus (below serious, 13 patients) Haematoma (below serious, 15 patients) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Cardiovascular injuries | 3.4% | 0.7 mg/kg 1 times / day multiple, intravenous Recommended Dose: 0.7 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 0.7 mg/kg, 1 times / day Sources: Page: p. 27 |
unhealthy, 39 years (range: 21-68 years) n = 87 Health Status: unhealthy Age Group: 39 years (range: 21-68 years) Sex: M+F Population Size: 87 Sources: Page: p. 27 |
Nervous system disorder NOS | 3.4% | 0.7 mg/kg 1 times / day multiple, intravenous Recommended Dose: 0.7 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 0.7 mg/kg, 1 times / day Sources: Page: p. 27 |
unhealthy, 39 years (range: 21-68 years) n = 87 Health Status: unhealthy Age Group: 39 years (range: 21-68 years) Sex: M+F Population Size: 87 Sources: Page: p. 27 |
Creatinine increased | 3.4% Disc. AE |
0.7 mg/kg 1 times / day multiple, intravenous Recommended Dose: 0.7 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 0.7 mg/kg, 1 times / day Sources: Page: p. 27 |
unhealthy, 39 years (range: 21-68 years) n = 87 Health Status: unhealthy Age Group: 39 years (range: 21-68 years) Sex: M+F Population Size: 87 Sources: Page: p. 27 |
Nausea | below serious, 118 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Depression | below serious, 12 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hypomagnesaemia | below serious, 12 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Pruritus | below serious, 13 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Weight decreased | below serious, 13 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Dyspepsia | below serious, 14 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Fluid retention | below serious, 15 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Haematoma | below serious, 15 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Oedema | below serious, 15 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Pneumonia | below serious, 15 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Blood bilirubin increased | below serious, 16 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Alopecia | below serious, 17 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Chest pain | below serious, 18 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hypocalcaemia | below serious, 18 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Aspartate aminotransferase increased | below serious, 19 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Erythema | below serious, 19 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Blood creatinine increased | below serious, 20 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Oral herpes | below serious, 22 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hypoalbuminaemia | below serious, 24 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Back pain | below serious, 34 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Abdominal pain upper | below serious, 39 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Rash | below serious, 39 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Thrombocytopenia | below serious, 42 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Oedema peripheral | below serious, 56 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hypokalaemia | below serious, 83 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Anaemia | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Back pain | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Bile duct stone | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Bronchospasm | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Cardio-respiratory arrest | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Cerebrovascular accident | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Chills | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Cholecystitis acute | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Cholecystitis | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Clostridium difficile colitis | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Drug hypersensitivity | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Dyspnoea | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Encephalitis | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Encephalopathy hepatic | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Enterococcal bacteraemia | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Gastroenteritis | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hepatic steatosis | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hepatocellular injury | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hyperbilirubinaemia | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hyperglycaemia | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hypersensitivity | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hyponatraemia | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hypotension | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Ileus | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Infection staphylococcal | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Intestinal obstruction | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Joint swelling | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Liver disorder | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Lymphocyte count decreased | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Metastases to central nervous system | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Mucosal inflammation | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Multi-organ failure | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Neutropenia | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Pancytopenia | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Pneumothorax | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Rash papular | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Renal tubular necrosis | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Respiratory distress | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Streptococcal sepsis | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Upper gastrointestinal haemorrhage | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Vomiting | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
White blood cell count decreased | serious, 1 patient | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Septic shock | serious, 13 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Acute respiratory distress syndrome | serious, 2 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Creatinine renal clearance decreased | serious, 2 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hepatic failure | serious, 2 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Hypokalaemia | serious, 2 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Pancreatitis | serious, 2 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Thrombocytopenia | serious, 2 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Blood creatinine increased | serious, 3 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Device related infection | serious, 3 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Cardiac arrest | serious, 4 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Pneumonia | serious, 7 patients | 5 mg/kg 2 times / week steady, intravenous Dose: 5 mg/kg, 2 times / week Route: intravenous Route: steady Dose: 5 mg/kg, 2 times / week Sources: |
unhealthy n = 237 Health Status: unhealthy Condition: Acute Lymphoblastic Leukemia Population Size: 237 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://aac.asm.org/content/60/6/3372.short Page: 3377.0 |
no | |||
Sources: https://aac.asm.org/content/60/6/3372.short Page: 3377.0 |
no | |||
Sources: https://aac.asm.org/content/60/6/3372.short Page: 3377.0 |
no | |||
Sources: https://aac.asm.org/content/60/6/3372.short Page: 3377.0 |
no | |||
Sources: https://aac.asm.org/content/60/6/3372.short Page: 3377.0 |
no | |||
Sources: https://aac.asm.org/content/60/6/3372.short Page: 3377.0 |
no | |||
Sources: https://aac.asm.org/content/58/10/5650.short Page: abstract |
no | |||
Sources: https://aac.asm.org/content/60/6/3372.short Page: 3377.0 |
no | |||
Sources: https://aac.asm.org/content/60/6/3372.short Page: abstract |
weak [IC50 127 uM] | |||
Sources: https://aac.asm.org/content/58/10/5650.short Page: abstract |
yes [IC50 7.6 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://aac.asm.org/content/58/8/4464.short Page: abstract |
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 1.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Combined activity of amphotericin B and 5-fluorocytosine against Cryptococcus neoformans in vitro and in vivo in mice. | 1975 Feb |
|
Mitigation of amphotericin B nephrotoxicity by mannitol. | 1975 Mar 8 |
|
[Drug-induced benign intracranial hypertension. Apropos of a case with amphotericin B. Review of the literature]. | 1992 Sep-Oct |
|
Recent strategies for the chemotherapy of visceral leishmaniasis. | 1999 Dec |
|
Risk factors for amphotericin B-induced nephrotoxicity. | 1999 Feb |
|
[Hypokalemia induced by amphotericin B]. | 1999 Nov 15 |
|
Fluconazole vs low-dose amphotericin B for the prevention of fungal infections in patients undergoing bone marrow transplantation: a study of the North American Marrow Transplant Group. | 2000 Apr |
|
Use of amphotericin B colloidal dispersion in children. | 2000 May-Jun |
|
[Renal failure during treatment with Ambisome]. | 2000 Oct 7 |
|
Role of humoral mediators in, and influence of a liposomal formulation on, acute amphotericin B nephrotoxicity. | 2001 Apr |
|
[Pulmonary mucormycosis: benefit of aerosol amphotericin B?]. | 2001 Jun |
|
Correlates of acute renal failure in patients receiving parenteral amphotericin B. | 2001 Oct |
|
[Radioprotective and antineoplastic activity of polyene antibiotics combined with dimethyl sulfoxide]. | 2002 |
|
Antileishmanial drugs cause up-regulation of interferon-gamma receptor 1, not only in the monocytes of visceral leishmaniasis cases but also in cultured THP1 cells. | 2003 Apr |
|
In vitro activity of voriconazole, itraconazole, caspofungin, anidulafungin (VER002, LY303366) and amphotericin B against aspergillus spp. | 2003 Feb |
|
Persistent acute tubular toxicity after switch from conventional amphotericin B to liposomal amphotericin B (Ambisome). | 2003 Feb |
|
In vitro susceptibility of Aspergillus spp. clinical isolates to albendazole. | 2003 Jun |
|
Amphotericin B binds to amyloid fibrils and delays their formation: a therapeutic mechanism? | 2003 May 27 |
|
Single-dose liposomal amphotericin B in the treatment of visceral leishmaniasis in India: a multicenter study. | 2003 Sep 15 |
|
Fatal fat embolism following amphotericin B lipid complex injection. | 2004 Dec |
|
N-acetylcysteine ameliorates amphotericin-induced nephropathy in rats. | 2005 |
|
Efficacy and safety of amphotericin B lipid complex in 548 children and adolescents with invasive fungal infections. | 2005 Feb |
|
Corticosteroid induced Cryptococcus meningitis. | 2005 Jul |
|
Prediction of genotoxicity of chemical compounds by statistical learning methods. | 2005 Jun |
|
Reversible dilated cardiomyopathy associated with amphotericin B treatment. | 2005 May |
|
Study of renal safety in amphotericin B lipid complex-treated patients. | 2005 May 1 |
|
Use of Leishmania donovani field isolates expressing the luciferase reporter gene in in vitro drug screening. | 2005 Sep |
|
Visceral leishmaniasis (kala-azar)--the Bihar (India) perspective. | 2006 Jul |
|
Symptomatic relapse of HIV-associated cryptococcal meningitis after initial fluconazole monotherapy: the role of fluconazole resistance and immune reconstitution. | 2006 Oct 15 |
|
Invasive aspergillosis: is treatment with "inexpensive" amphotericin B cost saving if "expensive" voriconazole is only used on demand? | 2006 Sep 30 |
|
Treatment of Bolivian mucosal leishmaniasis with miltefosine. | 2007 Feb 1 |
|
Discovery of novel indazole-linked triazoles as antifungal agents. | 2007 Jun 15 |
|
Injectable paromomycin for Visceral leishmaniasis in India. | 2007 Jun 21 |
|
In vitro efficacy of corifungin against Acanthamoeba castellanii trophozoites and cysts. | 2014 |
Sample Use Guides
In Vivo Use Guide
Curator's Comment: Description was created based on several sources, including:
http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a0a54943-9ce4-4f3e-b681-a1a9144c16ce
The recommended concentration for intravenous infusion is 0.1 mg/mL (1mg/10mL). Amphotericin B for Injection should no be given in doses greater than 1.5 mg/kg.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/12663162 http://www.ncbi.nlm.nih.gov/pubmed/11801575
Curator's Comment: Amphotericin B exhibited species-specific concentration-dependent activity, with 50% effective concentrations (EC50s) ranging from 0.10 to 0.12 mg/ml for A. fumigatus, 0.36 to 0.53 mg/ml for A. terreus, 0.27 to ≥32 mg/ml for F. solani, 0.41 to 0.55 mg/ml for F. oxysporum, and 0.97 and 0.65 mg/ml for S. apiospermum and S. prolificans, respectively.
http://www.ncbi.nlm.nih.gov/pubmed/15728887
The best fungicidal activity is for Candida albicans, (MFC90 1 ug/ml) and the lowest for C.parapsilosis, C.tropicalis and C.glabrata (MFC90 16 ug/ml). Amphotericin B spectrum of activity in clinically important candidas (MIC90(mg/L)): 0.25 - 2. Amphotericin B spectrum of activity in clinically important moulds (MIC90(mg/L)): 0.25 - >16.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 19:29:00 GMT 2023
by
admin
on
Sat Dec 16 19:29:00 GMT 2023
|
Record UNII |
44WG8E9MTU
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Common Name | English | ||
|
Common Name | English |
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
23668620
Created by
admin on Sat Dec 16 19:29:00 GMT 2023 , Edited by admin on Sat Dec 16 19:29:00 GMT 2023
|
PRIMARY | |||
|
44WG8E9MTU
Created by
admin on Sat Dec 16 19:29:00 GMT 2023 , Edited by admin on Sat Dec 16 19:29:00 GMT 2023
|
PRIMARY | |||
|
58501-21-6
Created by
admin on Sat Dec 16 19:29:00 GMT 2023 , Edited by admin on Sat Dec 16 19:29:00 GMT 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
PARENT -> SALT/SOLVATE |
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|