Rx00195 - Pralatrexate


Name:
Pralatrexate
Rx ID:
Rx00195
Validation Level:
Phenomic Similarity:
0.542
Reference ID:
DB06813
Primary Indications:
Relapsed peripheral T-cell lymphoma; refractory peripheral T-cell lymphoma
Orphan Indications:
No annotated orphan indications.
Rare Indications:
Diffuse large B-cell lymphoma; follicular lymphoma; advanced transitional cell carcinoma of the urinary bladder; metastatic transitional cell carcinoma of the urinary bladder
Common Indications:
Relapsed peripheral T-cell lymphoma; refractory peripheral T-cell lymphoma
Pathways:
Antimetabolite Pathway - Folate Cycle, Pharmacodynamics; Gemcitabine Action Pathway; Gemcitabine Metabolism Pathway; Thiopurine Pathway, Pharmacokinetics/Pharmacodynamics; Methotrexate Pathway (Cancer ...Click to show more
Drug Interactions:
Belatacept; Celecoxib; Denosumab; Diclofenac; Diflunisal; Etodolac; Fenoprofen; Flurbiprofen; Ibuprofen; Indomethacin; ...
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Food Interactions:
No annotated food interactions in DrugBank.

Interactive 3D Model

Interactive Drug Target Network

Interactive Bipartite Drug Repurposing Graph

Rx00195
Primary Indication
Secondary Indication

Visualize Chemical Properties

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Disease prevalence from Electronic Health Records

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Disease A Disease B A∩B A∩¬B B∩¬A Odds-Ratio P-Value Adjusted P-Value
relapsed peripheral T-cell lymphoma refractory peripheral T-cell lymphoma 102 102 102 39558.078 0 0.0
refractory peripheral T-cell lymphoma relapsed peripheral T-cell lymphoma 102 102 102 39558.078 0 0.0

Chemical, Pharmacological and Biological Annotations


ATC Code:
L01BA05
Categories:
No categories annotated in DrugBank
ChEBI ID:
71223
KEGG Drug ID:
D05589
SMILE:
NC1=NC2=NC=C(CC(CC#C)C3=CC=C(C=C3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)N=C2C(N)=N1
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
Classification:
Kingdom:
Organic Compounds
Superclass:
Benzenoids
Class:
Benzene and Substituted Derivatives
Subclass:
Benzamides
Indication:
Treatment of relapsed or refractory peripheral T-cell lymphoma.
Pharmacodynamics:
Pralatrexate is a 10-deazaaminopterin analogue of methotrexate. Compared to methotrexate, pralatrexate binds to RTC-1 with 10-times the affinity and is a more potent substrate for FPGS. As a result, pralatrexate is better internalized and r...
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Description:
Pralatrexate is an antimetabolite for the treatment of relapsed or refractory peripheral T-cell lymphoma. It is more efficiently retained in cancer cells than methotrexate. FDA approved on September 24, 2009.
Mechanism:
The selectivity of pralatrexate for cancer cells is based upon the observation that cancer cells generally have an overexpression of reduced folate carrier protein-1 (RTC-1) compared to normal somatic cells. This carrier protein allows the ...
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Adsorption, Distribution, Metabolism, Excretion and Toxicity


Human Intestinal Absorption:
-
Blood Brain Barrier:
+
Caco-2 permeable:
-
P-glycoprotein substrate:
Substrate
P-glycoprotein inhibitor I:
Non-inhibitor
P-glycoprotein inhibitor II:
Non-inhibitor
Renal organic cation transporter:
Non-inhibitor
CYP450 2C9 substrate:
Non-inhibitor
CYP450 2D6 substrate:
Non-inhibitor
CYP450 2C19 substrate:
Non-inhibitor
CYP450 inhibitory promiscuity:
Low CYP Inhibitory Promiscuity
Ames test:
Non AMES toxic
Carcinogenicity:
Non-carcinogens
Biodegradation:
Not ready biodegradable
Rat acute toxicity:
2.6263 LD50, mol/kg
hERG inhibition (predictor I):
Weak inhibitor
hERG inhibition (predictor II):
Non-inhibitor

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Dudley Laboratory
Department of Genetics and Genomic Sciences
Icahn Institute for Genomics and Multiscale Biology
Icahn School of Medicine at Mount Sinai
One Gustave L. Levy Place, Box 1498
Manhattan, New York City, NY
repurposedb@dudleylab.org