Details
Stereochemistry | EPIMERIC |
Molecular Formula | C23H23N7O5 |
Molecular Weight | 477.4726 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=NC(N)=C2N=C(CC(CC#C)C3=CC=C(C=C3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=NC2=N1
InChI
InChIKey=OGSBUKJUDHAQEA-WMCAAGNKSA-N
InChI=1S/C23H23N7O5/c1-2-3-14(10-15-11-26-20-18(27-15)19(24)29-23(25)30-20)12-4-6-13(7-5-12)21(33)28-16(22(34)35)8-9-17(31)32/h1,4-7,11,14,16H,3,8-10H2,(H,28,33)(H,31,32)(H,34,35)(H4,24,25,26,29,30)/t14?,16-/m0/s1
Pralatrexate (PDX or 10-propargyl-10-deazaaminopterin) is a folate analogue that is internalised by the reduced folate carrier 1 (RFC-1) protein, and polyglutamylated by the enzyme folylpolyglutamyl synthetase (FPGS), resulting in accumulation of the antifolate. Pralatrexate, a methotrexate analogue, is intended as an inhibitor of dihydrofolate reductase (DHFR), an enzyme which
catalyses the reduction of dihydrofolic acid to tetrahydrofolic acid. Inhibition of DHFR leads to a depletion of intracellular reduced folate stores, thereby leading to a disruption of DNA synthesis. Preclinical studies in vitro and in models of B-cell lymphomas, T-cell lymphomas and NSCLC indicated that pralatrexate exhibited antitumor activity that was superior to the activity of other antifolates. FOLOTYN (pralatrexate injection) is indicated for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL202 |
45.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | FOLOTYN Approved UseFOLOTYN is indicated for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL). This indication is based on overall response rate. Clinical benefit such as improvement in progression-free survival or overall survival has not been demonstrated. FOLOTYN is a folate analog metabolic inhibitor indicated for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL). This indication is based on overall response rate. Clinical benefit such as improvement in progression-free survival or overall survival has not been demonstrated. (1) Launch Date1.25375034E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4.9 μg/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/16136310 |
40 mg/m² single, intravenous dose: 40 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: PROBENECID |
PRALATREXATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4.9 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/16136310 |
40 mg/m² single, intravenous dose: 40 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: PROBENECID |
PRALATREXATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.8 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/16136310 |
40 mg/m² single, intravenous dose: 40 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: PROBENECID |
PRALATREXATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
33% |
PRALATREXATE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
325 mg/m2 1 times / 2 weeks steady, intravenous Highest studied dose Dose: 325 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 325 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 55.3 years n = 3 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 55.3 years Sex: M+F Population Size: 3 Sources: |
DLT: Mucositis... Dose limiting toxicities: Mucositis (grade 3, 2 patients) Sources: |
30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Disc. AE: Mucositis, Thrombocytopenia... Other AEs: Gastrointestinal inflammation, Genitourinary tract infections and inflammations NEC... AEs leading to discontinuation/dose reduction: Mucositis (7%) Other AEs:Thrombocytopenia (5%) Mucositis (grade 5, 1 patient) Febrile neutropenia (grade 5, 1 patient) Gastrointestinal inflammation (grade 3, 17%) Gastrointestinal inflammation (grade 4, 4%) Genitourinary tract infections and inflammations NEC (grade 3, 17%) Genitourinary tract infections and inflammations NEC (grade 4, 4%) Thrombocytopenia (grade 4, 19%) Gastrointestinal inflammation (all grades, 70%) Sources: Genitourinary tract infections and inflammations NEC (all grades, 70%) Thrombocytopenia (all grades, 41%) Thrombocytopenia (grade 3, 14%) Nausea (all grades, 40%) Nausea (grade 3, 4%) Fatigue (all grades, 36%) Fatigue (grade 3, 5%) Fatigue (grade 4, 2%) Anemia (all grades, 34%) Anemia (grade 3, 15%) Anemia (grade 4, 2%) Constipation (all grades, 33%) Pyrexia (all grades, 32%) Pyrexia (grade 3, 1%) Pyrexia (grade 4, 1%) Edema (all grades, 30%) Edema (grade 3, 1%) Cough (all grades, 28%) Cough (grade 3, 1%) Epistaxis (all grades, 26%) Vomiting (all grades, 25%) Vomiting (grade 3, 2%) Neutropenia (all grades, 24%) Neutropenia (grade 3, 13%) Neutropenia (grade 4, 7%) Diarrhea (all grades, 21%) Diarrhea (grade 3, 2%) Dyspnea (all grades, 19%) Dyspnea (grade 3, 7%) Anorexia (all grades, 15%) Anorexia (grade 3, 3%) Hypokalemia (all grades, 15%) Hypokalemia (grade 3, 4%) Hypokalemia (grade 4, 1%) Rash (all grades, 15%) Pruritus (all grades, 14%) Pruritus (grade 3, 2%) Pharyngolaryngeal pain (all grades, 14%) Pharyngolaryngeal pain (grade 3, 1%) Alanine aminotransferase increased (all grades, 13%) Alanine aminotransferase increased (grade 3, 5%) Aspartate aminotransferase increased (all grades, 13%) Aspartate aminotransferase increased (grade 3, 5%) Transaminases increased (all grades, 13%) Transaminases increased (grade 3, 5%) Abdominal pain (all grades, 12%) Abdominal pain (grade 3, 4%) Pain in extremity (all grades, 12%) Back pain (all grades, 11%) Back pain (grade 3, 3%) Leukopenia (all grades, 11%) Leukopenia (grade 3, 3%) Leukopenia (grade 4, 4%) Night sweats (all grades, 11%) Asthenia (all grades, 10%) Asthenia (grade 3, 1%) Tachycardia (all grades, 10%) Upper respiratory tract infection (all grades, 10%) Upper respiratory tract infection (grade 3, 1%) |
270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
DLT: Mucositis... Disc. AE: Dyspnea... Other AEs: Fatigue, Back pain... Dose limiting toxicities: Mucositis (grade 3, 1 patient) AEs leading todiscontinuation/dose reduction: Dyspnea (grade 4, 6%) Other AEs:Fatigue (grade 3, 25%) Sources: Back pain (grade 3, 13%) Dehydration (grade 3, 6%) Headache (grade 3, 6%) Malaise (grade 3, 6%) Chest pain (non-cardiac) (grade 3, 6%) Odynophagia (grade 3, 6%) Hand-and-foot syndrome (grade 3, 6%) Pleural effusion (grade 3, 6%) Respiratory obstruction unspecified (grade 3, 6%) Small intestine obstruction (grade 3, 6%) |
45 mg/m2 1 times / week steady, intravenous Highest studied dose Dose: 45 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 45 mg/m2, 1 times / week Sources: |
unhealthy n = 11 Health Status: unhealthy Condition: relapsed or refractory NHL | HL Population Size: 11 Sources: |
DLT: Neutropenic fever, Neutropenia... Dose limiting toxicities: Neutropenic fever (1 patient) Sources: Neutropenia (1 patient) Low platelets (1 patient) Stomatitis (2 patients) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Mucositis | grade 3, 2 patients DLT |
325 mg/m2 1 times / 2 weeks steady, intravenous Highest studied dose Dose: 325 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 325 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 55.3 years n = 3 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 55.3 years Sex: M+F Population Size: 3 Sources: |
Thrombocytopenia | 5% Disc. AE |
30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Mucositis | 7% Disc. AE |
30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Asthenia | all grades, 10% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Tachycardia | all grades, 10% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Upper respiratory tract infection | all grades, 10% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Back pain | all grades, 11% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Leukopenia | all grades, 11% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Night sweats | all grades, 11% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Abdominal pain | all grades, 12% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Pain in extremity | all grades, 12% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Alanine aminotransferase increased | all grades, 13% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Aspartate aminotransferase increased | all grades, 13% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Transaminases increased | all grades, 13% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Pharyngolaryngeal pain | all grades, 14% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Pruritus | all grades, 14% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Anorexia | all grades, 15% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Hypokalemia | all grades, 15% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Rash | all grades, 15% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Dyspnea | all grades, 19% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Diarrhea | all grades, 21% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Neutropenia | all grades, 24% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Vomiting | all grades, 25% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Epistaxis | all grades, 26% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Cough | all grades, 28% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Edema | all grades, 30% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Pyrexia | all grades, 32% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Constipation | all grades, 33% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Anemia | all grades, 34% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Fatigue | all grades, 36% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Nausea | all grades, 40% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Thrombocytopenia | all grades, 41% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Gastrointestinal inflammation | all grades, 70% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Genitourinary tract infections and inflammations NEC | all grades, 70% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Asthenia | grade 3, 1% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Cough | grade 3, 1% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Edema | grade 3, 1% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Pharyngolaryngeal pain | grade 3, 1% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Pyrexia | grade 3, 1% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Upper respiratory tract infection | grade 3, 1% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Neutropenia | grade 3, 13% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Thrombocytopenia | grade 3, 14% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Anemia | grade 3, 15% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Gastrointestinal inflammation | grade 3, 17% Disc. AE |
30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Genitourinary tract infections and inflammations NEC | grade 3, 17% Disc. AE |
30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Diarrhea | grade 3, 2% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Pruritus | grade 3, 2% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Vomiting | grade 3, 2% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Anorexia | grade 3, 3% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Back pain | grade 3, 3% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Leukopenia | grade 3, 3% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Abdominal pain | grade 3, 4% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Hypokalemia | grade 3, 4% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Nausea | grade 3, 4% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Alanine aminotransferase increased | grade 3, 5% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Aspartate aminotransferase increased | grade 3, 5% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Fatigue | grade 3, 5% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Transaminases increased | grade 3, 5% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Dyspnea | grade 3, 7% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Hypokalemia | grade 4, 1% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Pyrexia | grade 4, 1% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Thrombocytopenia | grade 4, 19% Disc. AE |
30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Anemia | grade 4, 2% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Fatigue | grade 4, 2% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Leukopenia | grade 4, 4% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Gastrointestinal inflammation | grade 4, 4% Disc. AE |
30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Genitourinary tract infections and inflammations NEC | grade 4, 4% Disc. AE |
30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Neutropenia | grade 4, 7% | 30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Febrile neutropenia | grade 5, 1 patient Disc. AE |
30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Mucositis | grade 5, 1 patient Disc. AE |
30 mg/m2 1 times / week steady, intravenous Recommended|MTD Dose: 30 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 59.0 years (range: 21-85 years) n = 111 Health Status: unhealthy Condition: peripheral T-cell lymphoma Age Group: 59.0 years (range: 21-85 years) Sex: M+F Population Size: 111 Sources: |
Mucositis | grade 3, 1 patient DLT |
270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Back pain | grade 3, 13% | 270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Fatigue | grade 3, 25% | 270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Chest pain (non-cardiac) | grade 3, 6% | 270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Dehydration | grade 3, 6% | 270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Hand-and-foot syndrome | grade 3, 6% | 270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Headache | grade 3, 6% | 270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Malaise | grade 3, 6% | 270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Odynophagia | grade 3, 6% | 270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Pleural effusion | grade 3, 6% | 270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Respiratory obstruction unspecified | grade 3, 6% | 270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Small intestine obstruction | grade 3, 6% | 270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Dyspnea | grade 4, 6% Disc. AE |
270 mg/m2 1 times / 2 weeks steady, intravenous MTD Dose: 270 mg/m2, 1 times / 2 weeks Route: intravenous Route: steady Dose: 270 mg/m2, 1 times / 2 weeks Co-administed with:: vitamin B12(1 mg intramuscular every 8 to 10 weeks) Sources: folic acid(1 mg orally once daily) |
unhealthy, 60.7 years n = 16 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 60.7 years Sex: M+F Population Size: 16 Sources: |
Neutropenia | 1 patient DLT |
45 mg/m2 1 times / week steady, intravenous Highest studied dose Dose: 45 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 45 mg/m2, 1 times / week Sources: |
unhealthy n = 11 Health Status: unhealthy Condition: relapsed or refractory NHL | HL Population Size: 11 Sources: |
Neutropenic fever | 1 patient DLT |
45 mg/m2 1 times / week steady, intravenous Highest studied dose Dose: 45 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 45 mg/m2, 1 times / week Sources: |
unhealthy n = 11 Health Status: unhealthy Condition: relapsed or refractory NHL | HL Population Size: 11 Sources: |
Low platelets | 1 patient DLT, Disc. AE |
45 mg/m2 1 times / week steady, intravenous Highest studied dose Dose: 45 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 45 mg/m2, 1 times / week Sources: |
unhealthy n = 11 Health Status: unhealthy Condition: relapsed or refractory NHL | HL Population Size: 11 Sources: |
Stomatitis | 2 patients DLT, Disc. AE |
45 mg/m2 1 times / week steady, intravenous Highest studied dose Dose: 45 mg/m2, 1 times / week Route: intravenous Route: steady Dose: 45 mg/m2, 1 times / week Sources: |
unhealthy n = 11 Health Status: unhealthy Condition: relapsed or refractory NHL | HL Population Size: 11 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Drug as victim
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=74 Page: 74.0 |
PubMed
Title | Date | PubMed |
---|---|---|
A phase I clinical pharmacologic study of pralatrexate in combination with probenecid in adults with advanced solid tumors. | 2006 May |
|
Gateways to clinical trials. | 2007 Apr |
|
Novel therapies for cutaneous T-cell lymphomas. | 2008 Dec |
|
Optimizing chemotherapeutic strategies for peripheral T-cell lymphomas. | 2008 Dec |
|
Importance of early splenectomy in patients with hepatosplenic T-cell lymphoma and severe thrombocytopenia. | 2009 Jul |
|
Gateways to clinical trials. | 2009 Mar |
|
Response to hydralazine-valproate in a patient with mycosis fungoides. | 2010 |
|
Clinical trials for human T-cell lymphotropic virus type I-associated peripheral T-cell lymphoma in Japan. | 2010 Apr |
|
Novel agents in development for peripheral T-cell lymphoma. | 2010 Apr |
|
Pralatrexate - from bench to bedside. | 2010 Feb |
|
Cancer chemotherapy: targeting folic acid synthesis. | 2010 Nov 19 |
|
Folotyn (pralatrexate injection) for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma: U.S. Food and Drug Administration drug approval summary. | 2010 Oct 15 |
|
Safety and efficacy of pralatrexate in the management of relapsed or refractory peripheral T-cell lymphoma. | 2012 |
|
Antifolates in cancer therapy: structure, activity and mechanisms of drug resistance. | 2012 Aug |
|
Pralatrexate : evaluation of clinical efficacy and toxicity in T-cell lymphoma. | 2013 Mar |
|
Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis. | 2015 May 18 |
Patents
Sample Use Guides
The recommended dose of FOLOTYN (pralatrexate injection) is 30 mg/m2 administered as an intravenous push over 3 to 5 minutes once weekly for 6 weeks in 7-week cycles.
Supplement patients with vitamin B12 1 mg intramuscularly every 8-10 weeks and folic acid 1.0-1.25 mg orally on a daily basis.
Treatment interruption or dose reduction to 20 mg/m2 may be needed to manage adverse drug reactions.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12854905
Pralatrexate (PDX or 10-propargyl-10-deazaaminopterin) demonstrated cytotoxicity against five lymphoma cell lines RL (transformed follicular lymphoma), HT, SKI-DLBCL-1 (diffuse large B cell), Raji (Burkitt's), and Hs445 (Hodgkin's disease) with IC50 values of 3-5 nM
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C511
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EU-Orphan Drug |
EU/3/07/444
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NDF-RT |
N0000175584
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FDA ORPHAN DRUG |
260708
Created by
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LIVERTOX |
NBK547901
Created by
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NCI_THESAURUS |
C2153
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FDA ORPHAN DRUG |
268308
Created by
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WHO-ATC |
L01BA05
Created by
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FDA ORPHAN DRUG |
225306
Created by
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WHO-VATC |
QL01BA05
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FDA ORPHAN DRUG |
269008
Created by
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EMA ASSESSMENT REPORTS |
FOLOTYN (REFUSED: LYMPHOMA, T-CELL)
Created by
admin on Sat Dec 16 10:41:59 UTC 2023 , Edited by admin on Sat Dec 16 10:41:59 UTC 2023
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662019
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C2250
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DB06813
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146464-95-1
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7786
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71223
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100000126312
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A8Q8I19Q20
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QQ-31
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CHEMBL1201746
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DTXSID3048578
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m9091
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PRIMARY | Merck Index | ||
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C418863
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4117
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8560
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148121
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754230
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PRALATREXATE
Created by
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PRIMARY | |||
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6840
Created by
admin on Sat Dec 16 10:41:59 UTC 2023 , Edited by admin on Sat Dec 16 10:41:59 UTC 2023
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SUB32989
Created by
admin on Sat Dec 16 10:41:59 UTC 2023 , Edited by admin on Sat Dec 16 10:41:59 UTC 2023
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A8Q8I19Q20
Created by
admin on Sat Dec 16 10:41:59 UTC 2023 , Edited by admin on Sat Dec 16 10:41:59 UTC 2023
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