Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C29H39NO9.ClH |
Molecular Weight | 582.082 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.[H][C@@]12[C@H](OC(=O)[C@@](O)(CCCC(C)(C)O)CC(=O)OC)C(OC)=C[C@@]13CCCN3CCC4=CC5=C(OCO5)C=C24
InChI
InChIKey=RRNSZQVHVKGKOS-CALFFDBBSA-N
InChI=1S/C29H39NO9.ClH/c1-27(2,33)8-5-10-29(34,16-23(31)36-4)26(32)39-25-22(35-3)15-28-9-6-11-30(28)12-7-18-13-20-21(38-17-37-20)14-19(18)24(25)28;/h13-15,24-25,33-34H,5-12,16-17H2,1-4H3;1H/t24-,25-,28+,29-;/m1./s1
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C29H39NO9 |
Molecular Weight | 545.6213 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/23053254http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdfCurator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/?term=23790799
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23053254http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203585lbl.pdf
Curator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/?term=23790799
Omacetaxine mepesuccinate (trade name Synribo) formerly named as homoharringtonine or HHT, is a pharmaceutical drug substance that is indicated for treatment of chronic myeloid leukemia (CML). It is a natural ester of the alkaloid cephalotaxine from Cephalotaxus harringtonia, now manufactured by hemi-synthesis. It was approved by the US FDA in October 2012 for the treatment of adult patients with CML with resistance and/or intolerance to two or more tyrosine kinase inhibitors (TKIs). The mechanism of action of omacetaxine mepesuccinate has not been fully elucidated but includes inhibition of protein synthesis and is independent of direct Bcr-Abl binding. Omacetaxine mepesuccinate binds to the A-site cleft in the peptidyl-transferase center of the large ribosomal subunit from a strain of archaeabacteria. In vitro, omacetaxine mepesuccinate reduced protein levels of the Bcr Abl oncoprotein and Mcl-1, an anti-apoptotic Bcl-2 family member. Omacetaxine mepesuccinate showed activity in mouse models of wild-type and T315I mutated Bcr-Abl CML.
CNS Activity
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=3598625
Curator's Comment: Homoharringtonine (omacetaxine mepesuccinate) can penetrate into brain tumors. Generally tritiated homoharringtonine ([3H]HHT, 150 microCi, 430 micrograms) was administered intravenously to seven patients at varying times before surgical resection of malignant brain tumor. Plasma, urine, cerebrospinal fluid (CSF), and tumor specimens were obtained during surgery, and the concentrations of HHT, its major metabolite, and [3H]HHT equivalent were determined chromatographically and radiochemically. A major metabolite of HHT was detectable in the tumor specimens of all the patients.
Originator
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=23790799
Curator's Comment: Homoharringtonine (omacetaxine mepesuccinate ) and related compound esters of cephalotaxine were described first in 1970. Omacetaxine mepesuccinate has been marketed by IVAX International GmbH (Teva) under the trade name SYNRIBO approved by FDA in 2012.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P39023 Gene ID: 6122.0 Gene Symbol: RPL3 Target Organism: Homo sapiens (Human) |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | SYNRIBO Approved UseIndicated for the treatment of adult patients with chronic or accelerated phase chronic myeloid leukemia (CML) with resistance and/or intolerance to two or more tyrosine kinase inhibitors (TKI). This indication is based upon response rate.There are no trials verifying an improvement in disease-related symptoms or increased survival with SYNRIBO Launch Date2012 |
|||
Primary | SYNRIBO Approved UseIndicated for the treatment of adult patients with chronic or accelerated phase chronic myeloid leukemia (CML) with resistance and/or intolerance to two or more tyrosine kinase inhibitors (TKI). This indication is based upon response rate.There are no trials verifying an improvement in disease-related symptoms or increased survival with SYNRIBO Launch Date2012 |
|||
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
25.1 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23053254 |
1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered: |
[NO STEREO] OMACETAXINE MEPESUCCINATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
136.2 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23053254 |
1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered: |
[NO STEREO] OMACETAXINE MEPESUCCINATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
6.96 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23053254 |
1.25 mg/m² single, subcutaneous dose: 1.25 mg/m² route of administration: Subcutaneous experiment type: SINGLE co-administered: |
[NO STEREO] OMACETAXINE MEPESUCCINATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
5 mg/m2 1 times / day multiple, subcutaneous MTD Dose: 5 mg/m2, 1 times / day Route: subcutaneous Route: multiple Dose: 5 mg/m2, 1 times / day Sources: |
unhealthy, 57 years (range: 20–79 years) n = 12 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Age Group: 57 years (range: 20–79 years) Sex: M+F Population Size: 12 Sources: |
DLT: Haematemesis, Pulmonary aspergillosis... Other AEs: Anasarca... Dose limiting toxicities: Haematemesis (grade 3, 1 patient) Other AEs:Pulmonary aspergillosis (grade 4, 1 patient) Skin rash (grade 3, 1 patient) Scalp pain (grade 3, 1 patient) Anasarca (grade 3, 1 patient) Sources: |
3 mg/m2 1 times / day multiple, subcutaneous Dose: 3 mg/m2, 1 times / day Route: subcutaneous Route: multiple Dose: 3 mg/m2, 1 times / day Sources: |
unhealthy, 57 years (range: 20–79 years) n = 12 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Age Group: 57 years (range: 20–79 years) Sex: M+F Population Size: 12 Sources: |
DLT: Hyperglycaemia, Diabetic hyperosmolar coma... Dose limiting toxicities: Hyperglycaemia (grade 3, 1 patient) Sources: Diabetic hyperosmolar coma |
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Disc. AE: Thrombocytopenia, Alanine aminotransferase increased... Other AEs: Thrombocytopenia, Thrombocytopenia... AEs leading to discontinuation/dose reduction: Thrombocytopenia (2%) Other AEs:Alanine aminotransferase increased (2%) Thrombocytopenia (all grades, 74%) Sources: Thrombocytopenia (grade 3-4, 67%) Anemia (all grades, 61%) Anemia (grade 3-4, 36%) Neutropenia (all grades, 50%) Neutropenia (grade 3-4, 45%) Lymphopenia (all grades, 17%) Lymphopenia (grade 3-4, 16%) Bone marrow failure (all grades, 10%) Bone marrow failure (grade 3-4, 10%) Febrile neutropenia (all grades, 10%) Febrile neutropenia (grade 3-4, 10%) Diarrhea (all grades, 42%) Diarrhea (grade 3-4, 1%) Nausea (all grades, 32%) Nausea (grade 3-4, 1%) Constipation (grade 1-2, 15%) Abdominal pain upper (grade 1-2, 14%) Vomiting (grade 1-2, 12%) Fatigue (all grades, 26%) Fatigue (grade 3-4, 5%) Pyrexia (all grades, 24%) Pyrexia (grade 3-4, 1%) Asthenia (all grades, 23%) Asthenia (grade 3-4, 1%) Edema peripheral (grade 1-2, 13%) Infusion site reactions (grade 1-2, 34%) Arthralgia (all grades, 19%) Arthralgia (grade 3-4, 1%) Pain in extremity (all grades, 13%) Pain in extremity (grade 3-4, 1%) Back pain (all grades, 11%) Back pain (grade 3-4, 2%) Headache (all grades, 19%) Headache (grade 3-4, 1%) Insomnia (grade 1-2, 10%) Cough (all grades, 16%) Cough (grade 3-4, 1%) Epistaxis (all grades, 15%) Epistaxis (grade 3-4, 1%) Alopecia (grade 1-2, 15%) Rash (grade 1-2, 10%) |
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: Page: p. 57 |
unhealthy, 59 years n = 158 Health Status: unhealthy Condition: chronic phase, Accelerated Phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 158 Sources: Page: p. 57 |
Disc. AE: Bone marrow failure, Sepsis... AEs leading to discontinuation/dose reduction: Bone marrow failure (1%) Sources: Page: p. 57Sepsis (1%) Multiorgan failure (1%) Gout (1%) Renal failure (1%) |
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Other AEs: Anemia, Anemia... Other AEs: Anemia (all grades, 51%) Sources: Anemia (grade 3-4, 36%) Febrile neutropenia (all grades, 20%) Febrile neutropenia (grade 3-4, 16%) Neutropenia (all grades, 20%) Neutropenia (grade 3-4, 18%) Thrombocytopenia (all grades, 56%) Thrombocytopenia (grade 3-4, 49%) Diarrhea (all grades, 35%) Diarrhea (grade 3-4, 7%) Nausea (all grades, 27%) Nausea (grade 3-4, 4%) Vomiting (all grades, 15%) Vomiting (grade 3-4, 2%) Abdominal pain (grade 1-2, 13%) Fatigue (all grades, 31%) Fatigue (grade 3-4, 9%) Pyrexia (all grades, 29%) Pyrexia (grade 3-4, 2%) Asthenia (all grades, 24%) Asthenia (grade 3-4, 2%) Chills (grade 1-2, 13%) Infusion site reactions (grade 1-2, 22%) Anorexia (all grades, 13%) Anorexia (grade 3-4, 2%) Pain in extremity (all grades, 11%) Pain in extremity (grade 3-4, 2%) Headache (grade 1-2, 13%) Cough (grade 1-2, 15%) Dyspnea (all grades, 11%) Dyspnea (grade 3-4, 2%) Epistaxis (all grades, 11%) Epistaxis (grade 3-4, 2%) Bacterial infection (all grades, 56%) Bacterial infection (grade 3-4, 20%) Infection viral (all grades, 56%) Infection viral (grade 3-4, 20%) Fungal infection (all grades, 56%) Fungal infection (grade 3-4, 20%) Infection NOS (all grades, 56%) Infection NOS (grade 3-4, 20%) |
1.25 mg/m2 2 times / day steady, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: steady Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Disc. AE: Pancytopenia... AEs leading to discontinuation/dose reduction: Pancytopenia (2%) Sources: |
1.25 mg/m2 2 times / day steady, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: steady Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase CML Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Disc. AE: Alanine aminotransferase increased... AEs leading to discontinuation/dose reduction: Alanine aminotransferase increased (2%) Sources: |
1.25 mg/m2 2 times / day steady, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: steady Dose: 1.25 mg/m2, 2 times / day Sources: Page: p. 57 |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase CML Age Group: 59 years Sex: M+F Population Size: 108 Sources: Page: p. 57 |
Disc. AE: Tachyarrhythmia, Diplopia... AEs leading to discontinuation/dose reduction: Tachyarrhythmia (1%) Sources: Page: p. 57Diplopia (1%) |
8 mg/m2 1 times / day multiple, intravenous Highest studied dose Dose: 8 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 8 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: refractory malignancies Sources: |
DLT: Hypotension... |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: |
unhealthy n = 1 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Population Size: 1 Sources: |
Disc. AE: Gastrointestinal disorders, Gingival hemorrhage... AEs leading to discontinuation/dose reduction: Gastrointestinal disorders (1 patient) Sources: Gingival hemorrhage (1 patient) Alopecia (1 patient) Thrombocytopenia (grade 4, 1 patient) Neutropenia (grade 4, 1 patient) |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: Page: p. 67 |
unhealthy n = 1 Health Status: unhealthy Condition: CML Population Size: 1 Sources: Page: p. 67 |
Disc. AE: Gingival hemorrhage, Gastrointestinal disorders... AEs leading to discontinuation/dose reduction: Gingival hemorrhage (1 patient) Sources: Page: p. 67Gastrointestinal disorders (1 patient) Alopecia (1 patient) Thrombocytopenia (grade 4, 1 patient) Neutropenia (grade 4, 1 patient) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Anasarca | grade 3, 1 patient | 5 mg/m2 1 times / day multiple, subcutaneous MTD Dose: 5 mg/m2, 1 times / day Route: subcutaneous Route: multiple Dose: 5 mg/m2, 1 times / day Sources: |
unhealthy, 57 years (range: 20–79 years) n = 12 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Age Group: 57 years (range: 20–79 years) Sex: M+F Population Size: 12 Sources: |
Haematemesis | grade 3, 1 patient DLT |
5 mg/m2 1 times / day multiple, subcutaneous MTD Dose: 5 mg/m2, 1 times / day Route: subcutaneous Route: multiple Dose: 5 mg/m2, 1 times / day Sources: |
unhealthy, 57 years (range: 20–79 years) n = 12 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Age Group: 57 years (range: 20–79 years) Sex: M+F Population Size: 12 Sources: |
Scalp pain | grade 3, 1 patient DLT |
5 mg/m2 1 times / day multiple, subcutaneous MTD Dose: 5 mg/m2, 1 times / day Route: subcutaneous Route: multiple Dose: 5 mg/m2, 1 times / day Sources: |
unhealthy, 57 years (range: 20–79 years) n = 12 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Age Group: 57 years (range: 20–79 years) Sex: M+F Population Size: 12 Sources: |
Skin rash | grade 3, 1 patient DLT |
5 mg/m2 1 times / day multiple, subcutaneous MTD Dose: 5 mg/m2, 1 times / day Route: subcutaneous Route: multiple Dose: 5 mg/m2, 1 times / day Sources: |
unhealthy, 57 years (range: 20–79 years) n = 12 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Age Group: 57 years (range: 20–79 years) Sex: M+F Population Size: 12 Sources: |
Pulmonary aspergillosis | grade 4, 1 patient DLT |
5 mg/m2 1 times / day multiple, subcutaneous MTD Dose: 5 mg/m2, 1 times / day Route: subcutaneous Route: multiple Dose: 5 mg/m2, 1 times / day Sources: |
unhealthy, 57 years (range: 20–79 years) n = 12 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Age Group: 57 years (range: 20–79 years) Sex: M+F Population Size: 12 Sources: |
Diabetic hyperosmolar coma | DLT | 3 mg/m2 1 times / day multiple, subcutaneous Dose: 3 mg/m2, 1 times / day Route: subcutaneous Route: multiple Dose: 3 mg/m2, 1 times / day Sources: |
unhealthy, 57 years (range: 20–79 years) n = 12 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Age Group: 57 years (range: 20–79 years) Sex: M+F Population Size: 12 Sources: |
Hyperglycaemia | grade 3, 1 patient DLT |
3 mg/m2 1 times / day multiple, subcutaneous Dose: 3 mg/m2, 1 times / day Route: subcutaneous Route: multiple Dose: 3 mg/m2, 1 times / day Sources: |
unhealthy, 57 years (range: 20–79 years) n = 12 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Age Group: 57 years (range: 20–79 years) Sex: M+F Population Size: 12 Sources: |
Alanine aminotransferase increased | 2% Disc. AE |
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Thrombocytopenia | 2% Disc. AE |
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Bone marrow failure | all grades, 10% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Febrile neutropenia | all grades, 10% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Back pain | all grades, 11% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Pain in extremity | all grades, 13% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Epistaxis | all grades, 15% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Cough | all grades, 16% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Lymphopenia | all grades, 17% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Arthralgia | all grades, 19% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Headache | all grades, 19% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Asthenia | all grades, 23% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Pyrexia | all grades, 24% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Fatigue | all grades, 26% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Nausea | all grades, 32% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Diarrhea | all grades, 42% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Neutropenia | all grades, 50% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Anemia | all grades, 61% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Thrombocytopenia | all grades, 74% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Insomnia | grade 1-2, 10% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Rash | grade 1-2, 10% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Vomiting | grade 1-2, 12% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Edema peripheral | grade 1-2, 13% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Abdominal pain upper | grade 1-2, 14% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Alopecia | grade 1-2, 15% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Constipation | grade 1-2, 15% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Infusion site reactions | grade 1-2, 34% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Arthralgia | grade 3-4, 1% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Asthenia | grade 3-4, 1% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Cough | grade 3-4, 1% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Diarrhea | grade 3-4, 1% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Epistaxis | grade 3-4, 1% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Headache | grade 3-4, 1% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Nausea | grade 3-4, 1% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Pain in extremity | grade 3-4, 1% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Pyrexia | grade 3-4, 1% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Bone marrow failure | grade 3-4, 10% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Febrile neutropenia | grade 3-4, 10% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Lymphopenia | grade 3-4, 16% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Back pain | grade 3-4, 2% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Anemia | grade 3-4, 36% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Neutropenia | grade 3-4, 45% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Fatigue | grade 3-4, 5% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Thrombocytopenia | grade 3-4, 67% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Bone marrow failure | 1% Disc. AE |
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: Page: p. 57 |
unhealthy, 59 years n = 158 Health Status: unhealthy Condition: chronic phase, Accelerated Phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 158 Sources: Page: p. 57 |
Gout | 1% Disc. AE |
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: Page: p. 57 |
unhealthy, 59 years n = 158 Health Status: unhealthy Condition: chronic phase, Accelerated Phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 158 Sources: Page: p. 57 |
Multiorgan failure | 1% Disc. AE |
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: Page: p. 57 |
unhealthy, 59 years n = 158 Health Status: unhealthy Condition: chronic phase, Accelerated Phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 158 Sources: Page: p. 57 |
Renal failure | 1% Disc. AE |
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: Page: p. 57 |
unhealthy, 59 years n = 158 Health Status: unhealthy Condition: chronic phase, Accelerated Phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 158 Sources: Page: p. 57 |
Sepsis | 1% Disc. AE |
1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: Page: p. 57 |
unhealthy, 59 years n = 158 Health Status: unhealthy Condition: chronic phase, Accelerated Phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 158 Sources: Page: p. 57 |
Dyspnea | all grades, 11% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Epistaxis | all grades, 11% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Pain in extremity | all grades, 11% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Anorexia | all grades, 13% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Vomiting | all grades, 15% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Febrile neutropenia | all grades, 20% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Neutropenia | all grades, 20% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Asthenia | all grades, 24% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Nausea | all grades, 27% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Pyrexia | all grades, 29% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Fatigue | all grades, 31% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Diarrhea | all grades, 35% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Anemia | all grades, 51% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Bacterial infection | all grades, 56% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Fungal infection | all grades, 56% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Infection NOS | all grades, 56% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Infection viral | all grades, 56% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Thrombocytopenia | all grades, 56% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Abdominal pain | grade 1-2, 13% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Chills | grade 1-2, 13% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Headache | grade 1-2, 13% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Cough | grade 1-2, 15% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Infusion site reactions | grade 1-2, 22% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Febrile neutropenia | grade 3-4, 16% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Neutropenia | grade 3-4, 18% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Anorexia | grade 3-4, 2% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Asthenia | grade 3-4, 2% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Dyspnea | grade 3-4, 2% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Epistaxis | grade 3-4, 2% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Pain in extremity | grade 3-4, 2% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Pyrexia | grade 3-4, 2% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Vomiting | grade 3-4, 2% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Bacterial infection | grade 3-4, 20% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Fungal infection | grade 3-4, 20% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Infection NOS | grade 3-4, 20% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Infection viral | grade 3-4, 20% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Anemia | grade 3-4, 36% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Nausea | grade 3-4, 4% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Thrombocytopenia | grade 3-4, 49% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Diarrhea | grade 3-4, 7% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Fatigue | grade 3-4, 9% | 1.25 mg/m2 2 times / day multiple, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 55 Health Status: unhealthy Condition: Chronic Myeloid Leukemia – Accelerated Phase Age Group: 59 years Population Size: 55 Sources: |
Pancytopenia | 2% Disc. AE |
1.25 mg/m2 2 times / day steady, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: steady Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase chronic myeloid leukemia Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Alanine aminotransferase increased | 2% Disc. AE |
1.25 mg/m2 2 times / day steady, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: steady Dose: 1.25 mg/m2, 2 times / day Sources: |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase CML Age Group: 59 years Sex: M+F Population Size: 108 Sources: |
Diplopia | 1% Disc. AE |
1.25 mg/m2 2 times / day steady, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: steady Dose: 1.25 mg/m2, 2 times / day Sources: Page: p. 57 |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase CML Age Group: 59 years Sex: M+F Population Size: 108 Sources: Page: p. 57 |
Tachyarrhythmia | 1% Disc. AE |
1.25 mg/m2 2 times / day steady, subcutaneous Recommended Dose: 1.25 mg/m2, 2 times / day Route: subcutaneous Route: steady Dose: 1.25 mg/m2, 2 times / day Sources: Page: p. 57 |
unhealthy, 59 years n = 108 Health Status: unhealthy Condition: chronic phase CML Age Group: 59 years Sex: M+F Population Size: 108 Sources: Page: p. 57 |
Hypotension | DLT | 8 mg/m2 1 times / day multiple, intravenous Highest studied dose Dose: 8 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 8 mg/m2, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: refractory malignancies Sources: |
Alopecia | 1 patient Disc. AE |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: |
unhealthy n = 1 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Population Size: 1 Sources: |
Gastrointestinal disorders | 1 patient Disc. AE |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: |
unhealthy n = 1 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Population Size: 1 Sources: |
Gingival hemorrhage | 1 patient Disc. AE |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: |
unhealthy n = 1 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Population Size: 1 Sources: |
Neutropenia | grade 4, 1 patient Disc. AE |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: |
unhealthy n = 1 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Population Size: 1 Sources: |
Thrombocytopenia | grade 4, 1 patient Disc. AE |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: |
unhealthy n = 1 Health Status: unhealthy Condition: Chronic Myeloid Leukemia Population Size: 1 Sources: |
Alopecia | 1 patient Disc. AE |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: Page: p. 67 |
unhealthy n = 1 Health Status: unhealthy Condition: CML Population Size: 1 Sources: Page: p. 67 |
Gastrointestinal disorders | 1 patient Disc. AE |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: Page: p. 67 |
unhealthy n = 1 Health Status: unhealthy Condition: CML Population Size: 1 Sources: Page: p. 67 |
Gingival hemorrhage | 1 patient Disc. AE |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: Page: p. 67 |
unhealthy n = 1 Health Status: unhealthy Condition: CML Population Size: 1 Sources: Page: p. 67 |
Neutropenia | grade 4, 1 patient Disc. AE |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: Page: p. 67 |
unhealthy n = 1 Health Status: unhealthy Condition: CML Population Size: 1 Sources: Page: p. 67 |
Thrombocytopenia | grade 4, 1 patient Disc. AE |
2.5 mg/m2 2 times / day multiple, subcutaneous Overdose Dose: 2.5 mg/m2, 2 times / day Route: subcutaneous Route: multiple Dose: 2.5 mg/m2, 2 times / day Sources: Page: p. 67 |
unhealthy n = 1 Health Status: unhealthy Condition: CML Population Size: 1 Sources: Page: p. 67 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000ClinPharmR.pdf#page=20 Page: 20.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=61 Page: 61,56 |
strong [Inhibition 10 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=61 Page: 61,56 |
weak [Inhibition 10 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=61 Page: 61,56 |
weak [Inhibition 10 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=61 Page: 61,56 |
weak [Inhibition 10 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=61 Page: 61.0 |
weak |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=54 Page: 54.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000ClinPharmR.pdf#page=20 Page: 20.0 |
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203585Orig1s000PharmRedt.pdf#page=43 Page: 43.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Inhibition of protein synthesis in intact HeLa cells. | 1975 Oct |
|
Inhibition of translation in eukaryotic systems by harringtonine. | 1977 Jan |
|
Apoptotic response to homoharringtonine in human wt p53 leukemic cells is independent of reactive oxygen species generation and implicates Bax translocation, mitochondrial cytochrome c release and caspase activation. | 2001 Apr |
|
Formal intramolecular [5 + 2] photocycloaddition reactions of maleimides: a novel approach to the CDE ring skeleton of (-)-cephalotaxine. | 2001 Sep 20 |
|
A formal total synthesis of (+/-)-cephalotaxine using sequential N-acyliminium ion reactions. | 2002 Mar 21 |
|
Activity of drugs from traditional Chinese medicine toward sensitive and MDR1- or MRP1-overexpressing multidrug-resistant human CCRF-CEM leukemia cells. | 2002 Mar-Apr |
|
Molecular modes of action of cephalotaxine and homoharringtonine from the coniferous tree Cephalotaxus hainanensis in human tumor cell lines. | 2003 Jan |
|
Altering chemosensitivity by modulating translation elongation. | 2009 |
|
[Expression and function of Ahi-1 gene in Jurkat cells]. | 2009 Apr |
Substance Class |
Chemical
Created
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563OX5661H
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Record Status |
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