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Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Ametantrone (AM) is a synthetic 9,10-anthracenedione bearing two (hydroxyethylamino)ethylamino residues at positions 1 and 4; along with other anthraquinones and anthracyclines, it shares a polycyclic intercalating moiety and charged side chains that stabilize DNA binding. Ametantrone is anticancer drug candidate targeting DNA. Ametantrone is a topoisomerase II inhibitor of the anthrapyrazole family. Ametantrone induces interstrand DNA cross-links in HeLa S3 cells. These cross-links were observed only in cellular system suggesting that metabolism of the drugs is a necessary step leading to DNA cross-linking. Ametantrone appeared to be very well tolerated and easy to handle. A dose-schedule of 135 mg/m2 q 2–3 weeks was recommended for phase II studies in solid tumors.
Class (Stereo):
CHEMICAL (ACHIRAL)
Bufrolin is xanthine derivative and mast cell stabilizer with antiallergic activity. In recent studies, Bufrolin was found to be high potency agonists of human GPR35.
Status:
Investigational
Source:
NCT01097018: Phase 3 Interventional Completed Colorectal Cancer
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Perifosine is an orally active alkyl-phosphocholine compound with potential antineoplastic activity. Perifosine is an Akt inhibitor, which targets the pleckstrin homology domain of Akt, thereby preventing its translocation to the plasma membrane. Perifosine exerts Akt-dependent and Akt-independent effects, and although many preclinical studies have documented Akt inhibition by perifosine, clinical validation of these findings is lacking. Perifosine is in phase II and III clinical trials for the treatment of neuroblastoma, glioblastoma multiforme and other solid tumors.
Class (Stereo):
CHEMICAL (ACHIRAL)
Carbantel is imidoylurea derivative patented by pharmaceutical company Sterling Drug Inc. As anthelmintic agent.
Status:
Investigational
Source:
INN:fandosentan [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Fandosentan (CI 1034 or PD 180988) is an endothelin A receptor antagonist. It inhibits pulmonary vasoconstriction. Fandosentan was being developed for the treatment of chronic obstructive pulmonary disease and pulmonary hypertension.
Status:
Investigational
Source:
NCT00977067: Phase 1 Interventional Terminated Solid Cancers
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
GDC-0152 binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domains of cIAP1 and cIAP2. GDC-0152 promotes degradation of cIAP1, induce activation of caspase-3/7, and lead to decreased viability of breast cancer cells. GDC-0152 improves outcome in breast cancer and glioma xenografted mouse. GDC 0512 was in phase I development in the US for the treatment of cancer; however, Roche announced in their 2009 results presentation, that development of the agent has been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Tiplasinin (PAI-039) is an orally efficacious and selective plasminogen activator inhibitor-1 (PAI-1) inhibitor. Tiplasinin bound specifically to the active conformation of PAI-1 and exhibited reversible inactivation of PAI-1 in vitro. Tiplaxtinin exhibited in vivo oral efficacy in two different models of acute arterial thrombosis. The remarkable preclinical safety and metabolic stability profiles of tiplaxtinin led to advancing the compound to Phase-I clinical trial for Thrombosis, which was later discontinued.
Status:
Investigational
Source:
NCT00681239: Phase 3 Interventional Completed Epilepsy
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cismadinone is a progestogen steroid.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Clanobutin is a choleretic drug. It increases the secretion of bile by hepatocytes. Clanobutin sodium has been introduced as a choleretic and digestant agent for animals. It has been used in all domestic animals in which enhancement of digestion and all associated secretory processes are indicated. Clanobutin was reported to induce a demonstrable increase in the secretory activity of the exocrine digestive glands and in the excretion of the bile.