U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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
Structure of PRALATREXATE

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

HIDE SMILES / InChI

Molecular Formula C23H23N7O5
Molecular Weight 477.4726
Charge 0
Count
Stereochemistry EPIMERIC
Additional Stereochemistry No
Defined Stereocenters 1 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
45.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
FOLOTYN

Approved Use

FOLOTYN 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 Date

2009
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
4.9 μg/mL
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

AUC

ValueDoseCo-administeredAnalytePopulation
4.9 μg × h/mL
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

T1/2

ValueDoseCo-administeredAnalytePopulation
1.8 h
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

Funbound

ValueDoseCo-administeredAnalytePopulation
33%
PRALATREXATE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse 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)
folic acid(1 mg orally once daily)
Sources:
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%)
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%)
Other AEs:
Gastrointestinal inflammation (all grades, 70%)
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%)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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 to
discontinuation/dose reduction:
Dyspnea (grade 4, 6%)
Other AEs:
Fatigue (grade 3, 25%)
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%)
Sources:
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)
Neutropenia (1 patient)
Low platelets (1 patient)
Stomatitis (2 patients)
Sources:
AEs

AEs

AESignificanceDosePopulation
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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)
folic acid(1 mg orally once daily)
Sources:
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:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [Inhibition 100 uM]
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
yes
yes
yes
yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
The schedule-dependent effects of the novel antifolate pralatrexate and gemcitabine are superior to methotrexate and cytarabine in models of human non-Hodgkin's lymphoma.
2006 Feb 1
A phase I clinical pharmacologic study of pralatrexate in combination with probenecid in adults with advanced solid tumors.
2006 May
Gateways to clinical trials.
2006 Nov
Phase II trial of pralatrexate (10-propargyl-10-deazaaminopterin, PDX) in patients with unresectable malignant pleural mesothelioma.
2007 Apr
Pralatrexate, a novel class of antifol with high affinity for the reduced folate carrier-type 1, produces marked complete and durable remissions in a diversity of chemotherapy refractory cases of T-cell lymphoma.
2007 Nov
Pralatrexate, a dihydrofolate reductase inhibitor for the potential treatment of several malignancies.
2008 Jul
Pralatrexate, a new hope for aggressive T-cell lymphomas?
2009 Apr
A population pharmacokinetic and pharmacodynamic evaluation of pralatrexate in patients with relapsed or refractory non-Hodgkin's or Hodgkin's lymphoma.
2009 Aug
Importance of early splenectomy in patients with hepatosplenic T-cell lymphoma and severe thrombocytopenia.
2009 Jul
Novel therapies for peripheral T-cell non-Hodgkin's lymphomas.
2009 Jul
Pralatrexate-induced tumor cell apoptosis in the epidermis of a patient with HTLV-1 adult T-cell lymphoma/leukemia causing skin erosions.
2009 Jun 18
Gateways to clinical trials.
2009 Mar
FDA approves pralatrexate for treatment of rare lymphoma.
2009 Nov 1
Distinct mechanistic activity profile of pralatrexate in comparison to other antifolates in in vitro and in vivo models of human cancers.
2009 Oct
Phase II-I-II study of two different doses and schedules of pralatrexate, a high-affinity substrate for the reduced folate carrier, in patients with relapsed or refractory lymphoma reveals marked activity in T-cell malignancies.
2009 Sep 10
Response to hydralazine-valproate in a patient with mycosis fungoides.
2010
Gateways to clinical trials.
2010 Apr
Novel agents in development for peripheral T-cell lymphoma.
2010 Apr
New targets of therapy in T-cell lymphomas.
2010 Apr
A case of blastic plasmacytoid dendritic cell neoplasm initially mimicking cutaneous lupus erythematosus.
2010 Dec
The antifolates: evolution, new agents in the clinic, and how targeting delivery via specific membrane transporters is driving the development of a next generation of folate analogs.
2010 Dec
Targeting histone deacetyalses in the treatment of B- and T-cell malignancies.
2010 Dec
Pralatrexate - from bench to bedside.
2010 Feb
Current and emerging treatment strategies for cutaneous T-cell lymphoma.
2010 Feb 12
Pralatrexate: basic understanding and clinical development.
2010 Jul
Anticancer agents against malaria: time to revisit?
2010 Mar
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
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
Substance Class Chemical
Created
by admin
on Sat Dec 16 10:41:58 GMT 2023
Edited
by admin
on Sat Dec 16 10:41:58 GMT 2023
Record UNII
A8Q8I19Q20
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PRALATREXATE
DASH   HSDB   INN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
PRALATREXATE [MI]
Common Name English
PRALATREXATE [JAN]
Common Name English
PDX
Common Name English
Pralatrexate [WHO-DD]
Common Name English
PRALATREXATE [ORANGE BOOK]
Common Name English
NSC-754230
Code English
(2S)-2-[[4-[(1RS)-1-[(2,4-Diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl]amino]pentanedioic acid
Systematic Name English
PRALATREXATE [USAN]
Common Name English
L-GLUTAMIC ACID, N-(4-(1-((2,4-DIAMINO-6-PTERIDINYL)METHYL)-3-BUTYNYL)BENZOYL)-
Systematic Name English
PRALATREXATE [HSDB]
Common Name English
PRALATREXATE [MART.]
Common Name English
PRALATREXATE [VANDF]
Common Name English
FOLOTYN
Brand Name English
pralatrexate [INN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C511
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
EU-Orphan Drug EU/3/07/444
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
NDF-RT N0000175584
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
FDA ORPHAN DRUG 260708
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
LIVERTOX NBK547901
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
NCI_THESAURUS C2153
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
FDA ORPHAN DRUG 268308
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
WHO-ATC L01BA05
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
FDA ORPHAN DRUG 225306
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
WHO-VATC QL01BA05
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
FDA ORPHAN DRUG 269008
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
EMA ASSESSMENT REPORTS FOLOTYN (REFUSED: LYMPHOMA, T-CELL)
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
Code System Code Type Description
RXCUI
662019
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY RxNorm
NCI_THESAURUS
C2250
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
DRUG BANK
DB06813
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
CAS
146464-95-1
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
HSDB
7786
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
CHEBI
71223
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
SMS_ID
100000126312
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
DAILYMED
A8Q8I19Q20
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
USAN
QQ-31
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
ChEMBL
CHEMBL1201746
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
EPA CompTox
DTXSID3048578
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
MERCK INDEX
m9091
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY Merck Index
MESH
C418863
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
DRUG CENTRAL
4117
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
INN
8560
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
PUBCHEM
148121
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
NSC
754230
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
WIKIPEDIA
PRALATREXATE
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
IUPHAR
6840
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
EVMPD
SUB32989
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
FDA UNII
A8Q8I19Q20
Created by admin on Sat Dec 16 10:41:59 GMT 2023 , Edited by admin on Sat Dec 16 10:41:59 GMT 2023
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC