Delving into the Latest Updates on XL-820 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

XL 820, XL820

Target

PDGFRs x VEGFR2 x c-Kit

Action

antagonists, inhibitors

Mechanism

PDGFR antagonists(Platelet-derived growth factor receptor antagonists), VEGFR2 antagonists(Vascular endothelial growth factor receptor 2 antagonists), c-Kit inhibitors(Stem cell growth factor receptor inhibitors)

Therapeutic Areas

NeoplasmsDigestive System DisordersSkin and Musculoskeletal Diseases+ [1]

Active Indication-

Inactive Indication

Advanced Malignant Solid NeoplasmGastrointestinal Stromal Tumors

Originator Organization

Exelixis, Inc.

Active Organization-

Inactive Organization

Exelixis, Inc.

License Organization

Exelixis, Inc.

GSK Plc

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

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Gene expression profiles GSE44561, GSE48079 and GSE22772GSE48079GSE22772 of glioma cells samples with activated Notch signaling pathway and control samples were downloaded from Gene Expression Omnibus database to screen the differentially expressed genes (DEGs) using limma package. GO (Gene Oncology) function and KEGG (Kyoto Encyclopedia of Genes and Genomes) pathway enrichment analyses were conducted using DAVID tools to predict the underlying function of these DEGs. Sequentially, drug target genes recorded in DrugBank database were collected and matched with the selected DEGs to identify the potential drug targets for glioma. Further, these targets were verified by the screened DEGs in the anti-glioma drug (AT13148) treated samples of microarray data of GSE38008.

RESULTS:

A total of 75,645,497 DEGs were respectively identified in GSE44561, GSE48079 and GSE22772GSE48079GSE22772 datasets and these DEGs could well distinguish the glioma samples from controls. The DEGs were mainly enriched in classical functions and pathways, such as cell cycle, and DNA replication. A total of 122 DEGs were found to be potential drug targets for glioma, among which GLIPR1 was targeted by drug XL820, PDGFRB and KDR were targeted by SOT-107. Efficacy validation of the other 119 drug targets by GSE38008 data showed that ACSS1, ASL, GCLM, ROCK2, IMPA1, and TFPI may be targeted by the anti-glioma drug of AT13148.

CONCLUSION:

AT13148 may inhibit glioma progression by suppressing the Notch signaling genes, including GLIPR1, PDGFRB, ACSS1, and ASL.

01 Mar 2007·Methods and findings in experimental and clinical pharmacology

Gateways to clinical trials.

Author: Bayes, Miriam

Agomelatine, AGRO-100, AIDSVAX gp120 B/E, alfimeprase, aliskiren fumarate, ALVAC vCP1452, alvocidib hydrochloride, ambrisentan, AME-527, AN-0128, apadenoson, ARRY-142886, asenapine maleate, axitinib, azimilide hydrochloride; Belimumab, bevacizumab, biolimus A9, BiovaxID, bryostatin 1; Cannabidiol, celgosivir, CG-1940/CG-8711, CKD-501, collagen-PVP, CpG-10101, CTL-102, CTL-102/CB-1954; D-4F, darusentan, dexverapamil, DNA influenza vaccine, dronabinol/cannabidiol, dronedarone hydrochloride; Eculizumab, edodekin alfa, edotecarin, enzastaurin hydrochloride; Fingolimod hydrochloride; Golimumab; HBV-DNA vaccine, hyaluronic acid; I-131 ch-TNT-1/B, imatinib mesylate, inhaled insulin, ipilimumab, ispinesib mesylate, i.v. gamma-globulin; KU-59436; Lapaquistat; Mapatumumab, MC-1, MC-1/lisinopril, mepolizumab; Nibentan, nilotinib, Nobori, NV1FGF; Ocrelizumab; Paclimer, pagoclone, paliperidone, PC-515, PHA-794428, phosphostim, PPI-2458, prasugrel, PTC-299; Renzapride hydrochloride, Reolysin, reslizumab, revaprazan hydrochloride, rivaroxaban, romidepsin, rubitecan, ruboxistaurin mesilate hydrate; Sapacitabine, SarCNU, ST-1859, sunitinib malate; Tanespimycin, temsirolimus, tgAAC-94, TGN-255, ticagrelor, tipifarnib, tolvaptan, tretazicar, TRU-015; Upgrade varicella vaccine, Ushercell; Vernakalant hydrochloride, verpasep caltespen, VNP-40101M, VRC-HIVADV014-00-VP, VRC-HIVDNA009-00-VP, VX-001; XL-647, XL-820, XL-880, XL-999.

100 Deals associated with XL-820

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Gastrointestinal Stromal Tumors	Phase 2	United States	Exelixis, Inc.	01 Dec 2007
Advanced Malignant Solid Neoplasm	Phase 1	United States	Exelixis, Inc.	01 Aug 2005