U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Showing 1 - 10 of 2,588 results

Status:
US Approved Rx (2025)
First approved in 2025

Class (Stereo):
CHEMICAL (ABSOLUTE)



Treosulfan (l-threitol-1,4-bis-methanesulfonate; dihydroxybusulfan) is a prodrug of a bifunctional alkylating cytotoxic agent that is approved for the treatment of ovarian carcinomas in a number of European countries. The antitumor activity of treosu...
Status:
US Approved Rx (2024)
First approved in 2024

Class (Stereo):
CHEMICAL (ACHIRAL)



Xanomeline (LY-246,708) is an orthosteric muscarinic acetylcholine receptor (mAChR) agonist, often referred to as M1/M4-preferring. It is also known to act as a M5 receptor antagonist. Xanomeline was studied in clinical trials phase I in schizophreni...
Status:
US Approved Rx (2024)
First approved in 2024

Class (Stereo):
CHEMICAL (ACHIRAL)



Gavinostat is an orally bioavailable hydroxymate inhibitor of histone deacetylase (HDAC) with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. Gavinostat inhibits class I and class II HDACs, resulting in an accumulation of...
Status:
US Approved Rx (2024)
First approved in 2024

Class (Stereo):
CHEMICAL (ABSOLUTE)



X-396 (Ensartinib) is a novel, potent anaplastic lymphoma kinase (ALK) small molecule tyrosine kinase inhibitor (TKI) with additional activity against MET, ABL, Axl, EPHA2, LTK, ROS1 and SLK. Ensartinib has demonstrated activity in ALK treatment naïv...
Status:
US Approved Rx (2024)
First approved in 2024

Class (Stereo):
CHEMICAL (ABSOLUTE)



Vorasidenib (also known as AG 881) was developed as an isocitrate dehydrogenase (IDH) type 1 in the cytoplasm and type 2 in the mitochondria, with potential antineoplastic activity. It is known that IDH is an essential enzyme for cellular respiration...
Status:
US Approved Rx (2023)
First approved in 2023

Class (Stereo):
CHEMICAL (ACHIRAL)



Momelotinib (CYT387) is an ATP-competitive small molecule that potently inhibits JAK1/JAK2 kinases. Momelotinib is developing by Gilead Sciences for the oral treatment of pancreatic and non-small cell lung cancers, and myeloproliferative disorders (i...
Status:
US Approved Rx (2023)
First approved in 2023

Class (Stereo):
CHEMICAL (ABSOLUTE)



Elacestrant (ER-306323 or RAD 1901 [6R)-6-(2-(N-(4-(2-(ethylamino)ethyl)benzyl)-N-ethylamino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol dihydrochloride]) is an estrogen receptor antagonist that binds to estrogen receptor-alpha (ERα). In ERpo...
Status:
US Approved Rx (2022)
First approved in 2022

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Pacritinib (SB1518), discovered in Singapore at the labs of S*BIO Pte Ltd., is an oral tyrosine kinase inhibitor (TKI) with activity against two important activating mutations: Janus Associated Kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). T...
Status:
US Approved Rx (2022)
First approved in 2022

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Adagrasib (KRAZATI™) is an orally available, potent, small molecule inhibitor of KRAS G12C mutant isoform being developed by Mirati Therapeutics for the treatment of solid tumours harbouring KRAS G12C oncogenic driver mutation, including non-small ce...
Status:
US Approved Rx (2022)
First approved in 2022

Class (Stereo):
CHEMICAL (ABSOLUTE)



Olutasidenib (FT-2102) is a highly potent, orally bioavailable, brain-penetrant, and selective inhibitor of mutant IDH1. Olutasidenib was designed to reduce R-2-HG and revert pathologic epigenetic modifications that impair cellular differentiation to...