Id |
Subject |
Object |
Predicate |
Lexical cue |
T409 |
0-4 |
Sentence |
denotes |
4.7. |
T410 |
5-24 |
Sentence |
denotes |
Leflunomide (Arava) |
T411 |
25-111 |
Sentence |
denotes |
It is a synthetic, small molecule and an isoxazole-carboxamide derivative (Figure 8B). |
T412 |
112-139 |
Sentence |
denotes |
It was approved by the U.S. |
T413 |
140-213 |
Sentence |
denotes |
FDA in 1998 for the oral treatment of rheumatoid arthritis [173,174,175]. |
T414 |
214-420 |
Sentence |
denotes |
It is also used off-label as a replacement therapy in kidney transplant recipients with polyomavirus BK [176] and for cytomegalovirus disease in transplant recipients resistant to standard antivirals [177]. |
T415 |
421-523 |
Sentence |
denotes |
Mechanistically, it is a disease-modifying agent with anti-inflammatory and antiproliferative effects. |
T416 |
524-702 |
Sentence |
denotes |
It inhibits pyrimidine synthesis by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase, an important enzyme in the de novo synthesis of uridine monophosphate [178]. |
T417 |
703-842 |
Sentence |
denotes |
Leflunomide is a prodrug and the active metabolite (isoxazole ring is open: teriflunomide (Aubagio)) is responsible for its activity [179]. |
T418 |
843-904 |
Sentence |
denotes |
It inhibits rapidly dividing cells such as activated T cells. |
T419 |
905-968 |
Sentence |
denotes |
It has also been found to block the transcription factor NF-κB. |
T420 |
969-1010 |
Sentence |
denotes |
It also inhibits tyrosine kinase enzymes. |
T421 |
1011-1182 |
Sentence |
denotes |
The drug inhibits the replication of cytomegalovirus, herpes simplex virus 1, and polyomavirus BK by interfering with nucleocapsid tegumentation and virion assembly [179]. |
T422 |
1183-1377 |
Sentence |
denotes |
Given the above activities, a high dose of leflunomide is being evaluated for the treatment of ambulatory patients with mild COVID-19 at the University of Chicago Medicine (NCT04361214; n = 20). |