PRALATREXATE

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 Search

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

Description
Sources: https://www.tga.gov.au/sites/default/files/auspar-pralatrexate-130822.pdf | https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022468lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/18600598

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

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Dihydrofolate reductase 61 Target ID: CHEMBL202 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022468lbl.pdf	Inhibitor 8504		45.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Peripheral T-cell lymphoma (relapsed or refractory) 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022468lbl.pdf	Primary		Approved 8583	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

C_max

Value	Dose	Co-administered	Analyte	Population
3422.73 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/38029357/	30 mg/m² single, intravenous dose: 30 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:		PRALATREXATE, (S)- plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
3951.67 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/38029357/	30 mg/m² single, intravenous dose: 30 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:		PRALATREXATE, (R)- plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
5.3 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	PROBENECID	PRALATREXATE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
1857.11 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/38029357/	30 mg/m² single, intravenous dose: 30 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:		PRALATREXATE, (S)- plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
3363.28 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/38029357/	30 mg/m² single, intravenous dose: 30 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:		PRALATREXATE, (R)- plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
5.5 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	PROBENECID	PRALATREXATE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
4.49 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/38029357/	30 mg/m² single, intravenous dose: 30 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:		PRALATREXATE, (S)- plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
4.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/38029357/	30 mg/m² single, intravenous dose: 30 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:		PRALATREXATE, (R)- plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
2.5 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	PROBENECID	PRALATREXATE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
33% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022468s009lbl.pdf			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 Sources: https://pubmed.ncbi.nlm.nih.gov/21841501	unhealthy, 55.3 years Health Status: unhealthy Age Group: 55.3 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/21841501	DLT: Mucositis... Dose limiting toxicities: Mucositis (grade 3, 2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/21841501
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022468lbl.pdf	unhealthy, 59.0 years (range: 21-85 years) Health Status: unhealthy Age Group: 59.0 years (range: 21-85 years) Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022468lbl.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022468lbl.pdf
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 Sources: https://pubmed.ncbi.nlm.nih.gov/21841501	unhealthy, 60.7 years Health Status: unhealthy Age Group: 60.7 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/21841501	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: https://pubmed.ncbi.nlm.nih.gov/21841501
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: https://pubmed.ncbi.nlm.nih.gov/19652067	unhealthy Health Status: unhealthy Sources: https://pubmed.ncbi.nlm.nih.gov/19652067	DLT: Neutropenic fever, Neutropenia... Dose limiting toxicities: Neutropenic fever (1 patient) Neutropenia (1 patient) Low platelets (1 patient) Stomatitis (2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/19652067

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252 inducer 1087	substrate 1193 inhibitor 2438	substrate 1388 inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1741 CYP1A2 2153 CYP2A6 879 CYP2C8 1057 CYP2C19 2057 CYP2E1 1060 MRP2 499 MRP3 246 OCT2 779 OAT1 725 OAT3 747 OATP1B3 961 OATP1B1 1079 BCRP 910	P-gp 2052 CYP1A2 1197 CYP2A6 626 CYP2B6 776 CYP2C8 810 CYP2C19 1119 OCT2 434 BCRP 697 MRP2 252 MRP3 58 OATP1B3 435 OATP1B1 503 OAT1 395 OAT3 391	CYP1A2 832 CYP2C19 329

Drug as perpetrator

Target	Modality	Activity
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=30 Page: 30.0	no [Inhibition 100 uM]
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=30 Page: 30.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=30 Page: 30.0	no
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=30 Page: 30.0	no
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=30 Page: 30.0	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=30 Page: 30.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=30 Page: 30.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=30 Page: 30.0	no
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=30 Page: 30.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=30 Page: 30.0	no
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=30 Page: 30.0	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=6 Page: 6.0	no
MRP2 625	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	yes
MRP3 326	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	yes

Drug as victim

Target	Modality	Activity
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=19 Page: 19.0	no
CYP2A6 626	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=19 Page: 19.0	no
CYP2B6 776	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=19 Page: 19.0	no
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=19 Page: 19.0	no
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=19 Page: 19.0	no
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=19 Page: 19.0	no
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=19 Page: 19.0	no
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=19 Page: 19.0	no
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=19 Page: 19.0	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=6 Page: 6.0	no
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	yes
MRP2 252	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	yes
MRP3 58	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	yes
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022468s013lbl.pdf#page=9 Page: 9.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022468s000_ClinPharmR.pdf#page=74 Page: 74.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:71223	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:71223
ChemicalBook	CB31856065	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB31856065
MolPort	MolPort-009-679-397	https://www.molport.com/shop/molecule-link/MolPort-009-679-397
Selleck Chemicals	Pralatrexate(Folotyn)	http://www.selleckchem.com/products/Pralatrexate(Folotyn).html

PubMed

Title	Date	PubMed
Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis.	2015-05-18	25811541
Pralatrexate : evaluation of clinical efficacy and toxicity in T-cell lymphoma.	2013-03	23409799
Antifolates in cancer therapy: structure, activity and mechanisms of drug resistance.	2012-08	22921318
Safety and efficacy of pralatrexate in the management of relapsed or refractory peripheral T-cell lymphoma.	2012	23032692
A case of blastic plasmacytoid dendritic cell neoplasm initially mimicking cutaneous lupus erythematosus.	2010-12	21253327
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.	2010-12	21154123
Targeting histone deacetyalses in the treatment of B- and T-cell malignancies.	2010-12	21132350
Cancer chemotherapy: targeting folic acid synthesis.	2010-11-19	21301589
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.	2010-10-15	20739433
Pralatrexate is synergistic with the proteasome inhibitor bortezomib in in vitro and in vivo models of T-cell lymphoid malignancies.	2010-07-15	20501616
Pralatrexate (Folotyn) for peripheral T-cell lymphoma.	2010-07-12	20622807
Pralatrexate: basic understanding and clinical development.	2010-07	20509772
Primary cutaneous and systemic anaplastic large cell lymphoma: clinicopathologic aspects and therapeutic options.	2010-06	20669794
Gateways to clinical trials.	2010-04	20448862
Clinical trials for human T-cell lymphotropic virus type I-associated peripheral T-cell lymphoma in Japan.	2010-04	20359583
Novel agents in development for peripheral T-cell lymphoma.	2010-04	20359580
New targets of therapy in T-cell lymphomas.	2010-04	20196721
Anticancer agents against malaria: time to revisit?	2010-03	20056487
Current and emerging treatment strategies for cutaneous T-cell lymphoma.	2010-02-12	20166766
Pralatrexate - from bench to bedside.	2010-02	20393637
Peripheral T-cell lymphoma: review and updates of current management strategies.	2010	21234357
An update in management of noncutaneous T-cell lymphomas.	2010	21188274
Response to hydralazine-valproate in a patient with mycosis fungoides.	2010	20339522
FDA approves pralatrexate for treatment of rare lymphoma.	2009-11-01	19850775
Distinct mechanistic activity profile of pralatrexate in comparison to other antifolates in in vitro and in vivo models of human cancers.	2009-10	19221750
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.	2009-09-10	19652067
A population pharmacokinetic and pharmacodynamic evaluation of pralatrexate in patients with relapsed or refractory non-Hodgkin's or Hodgkin's lymphoma.	2009-08	19474785
Importance of early splenectomy in patients with hepatosplenic T-cell lymphoma and severe thrombocytopenia.	2009-07	19408055
Novel therapies for peripheral T-cell non-Hodgkin's lymphomas.	2009-07	19367159
Pralatrexate-induced tumor cell apoptosis in the epidermis of a patient with HTLV-1 adult T-cell lymphoma/leukemia causing skin erosions.	2009-06-18	19389878
Pralatrexate, a new hope for aggressive T-cell lymphomas?	2009-04	19380298
Gateways to clinical trials.	2009-03	19455266
Novel therapies for cutaneous T-cell lymphomas.	2008-12	19073526
Optimizing chemotherapeutic strategies for peripheral T-cell lymphomas.	2008-12	19073525
Pralatrexate, a dihydrofolate reductase inhibitor for the potential treatment of several malignancies.	2008-07	18600598
Gateways to clinical trials.	2008-05	18773127
CD4+ CD56+ hematodermic/plasmacytoid dendritic cell tumor with response to pralatrexate.	2008-03	18280345
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.	2007-11	17910632
Management of advanced-stage peripheral T-cell lymphomas.	2007-10	20425376
A phase 1 study of pralatrexate in combination with paclitaxel or docetaxel in patients with advanced solid tumors.	2007-05-01	17473201
Gateways to clinical trials.	2007-04	17520107
Phase II trial of pralatrexate (10-propargyl-10-deazaaminopterin, PDX) in patients with unresectable malignant pleural mesothelioma.	2007-04	17409804
Gateways to clinical trials.	2006-11	17200730
Pralatrexate: an emerging new agent with activity in T-cell lymphomas.	2006-11	16988580
New drugs for the treatment of advanced-stage diffuse large cell lymphomas.	2006-10	17027659
A phase I clinical pharmacologic study of pralatrexate in combination with probenecid in adults with advanced solid tumors.	2006-05	16136310
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.	2006-02-01	16467107

Patents

Sample Use Guides

In Vivo Use Guide

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

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 `Mon Mar 31 23:24:04 GMT 2025` Edited by `admin` on `Mon Mar 31 23:24:04 GMT 2025`
Record UNII	A8Q8I19Q20
Record Status	`Validated (UNII)`
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Name

Type

Language

PRALATREXATE

Official Name

English

FOLOTYN

Preferred 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

pralatrexate [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C511