U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 4181 - 4190 of 4747 results

Status:
Investigational
Source:
NCT04032080: Phase 2 Interventional Completed Triple Negative Breast Cancer
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



LY2606368 (Prexasertib) is a small-molecule Chk-1 inhibitors invented by Array and being developed by Eli Lilly and Company. Lilly is responsible for all clinical development and commercialization activities. LY2606368 is advancing in Phase 2 clinical trials for cancer. Prexasertib preferentially binds to and inhibits CHK1 and, to a lesser extent, inhibits CHK2. Chk-1 is a protein kinase that regulates the tumor cell's response to DNA damage often caused by treatment with chemotherapy. In response to DNA damage, Chk-1 blocks cell cycle progression in order to allow for repair of damaged DNA, thereby limiting the efficacy of chemotherapeutic agents. Inhibiting Chk-1 in combination with chemotherapy can enhance tumor cell death by preventing these cells from recovering from DNA damage.
Status:
Investigational
Source:
NCT00363454: Phase 1 Interventional Completed Cancer
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Triciribine is a purine analogue which inhibits DNA and protein synthesis, it is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2 and -3 but does not inhibit Akt kinase activity nor known upstream Akt activators such as PI 3-Kinase and PDK1. It inhibits cell growth and induces apoptosis preferentially in cells that express aberrant Akt1. In whole cells triciribine is phosphorylated by adenosine kinase which may be necessary for its activity. Triciribine is a cancer drug which was first synthesised in the 1970s and trialled clinically in the 1980s and 1990s without success. Following the discovery in the early 2000s that the drug would be effective against tumours with hyperactivated Akt, it is now again under consideration in a variety of cancers. As PTX-200, the drug is currently in two early stage clinical trials in breast cancer and ovarian cancer being conducted by the small molecule drug development company Prescient Therapeutics.
PHA-793887 is an inhibitor of multiple cyclin dependent kinases (CDK) with activity against CDK2, CDK1 and CDK4. PHA-793887 was cytotoxic for leukemic cell lines in vitro, with IC(50) ranging from 0.3 to 7 uM. In colony assays PHA-793887 showed very high activity against leukemia cell lines, with an IC(50) <0.1 uM indicating that it has efficient and prolonged antiproliferative activity. PHA-793887 induced cell-cycle arrest, inhibited Rb and nucleophosmin phosphorylation. PHA-793887 has promising therapeutic activity against acute leukemias in vitro and in vivo.
Status:
Investigational
Source:
NCT03641313: Phase 2 Interventional Active, not recruiting Clinical Stage III Gastric Cancer AJCC v8
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



VX-970 (VE-822) is an ATR kinase inhibitor. VE-822 decreased maintenance of cell-cycle checkpoints, increased persistent DNA damage and decreased homologous recombination in irradiated cancer cells. Vertex Pharmaceuticals is developing VX 970 for the treatment of advanced solid tumours. Phase I/II development is underway in the US for small-cell lung cancer and in the UK for solid tumours. Phase II development of VX 970 as a combination therapy in urogenital cancer, ovarian, primary peritoneal and fallopian tube cancer indications is underway in the US.
Status:
Investigational
Source:
NCT04032080: Phase 2 Interventional Completed Triple Negative Breast Cancer
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



LY2606368 (Prexasertib) is a small-molecule Chk-1 inhibitors invented by Array and being developed by Eli Lilly and Company. Lilly is responsible for all clinical development and commercialization activities. LY2606368 is advancing in Phase 2 clinical trials for cancer. Prexasertib preferentially binds to and inhibits CHK1 and, to a lesser extent, inhibits CHK2. Chk-1 is a protein kinase that regulates the tumor cell's response to DNA damage often caused by treatment with chemotherapy. In response to DNA damage, Chk-1 blocks cell cycle progression in order to allow for repair of damaged DNA, thereby limiting the efficacy of chemotherapeutic agents. Inhibiting Chk-1 in combination with chemotherapy can enhance tumor cell death by preventing these cells from recovering from DNA damage.
Status:
Investigational
Source:
NCT01415297: Phase 1 Interventional Completed Solid Tumors
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT04032080: Phase 2 Interventional Completed Triple Negative Breast Cancer
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



LY2606368 (Prexasertib) is a small-molecule Chk-1 inhibitors invented by Array and being developed by Eli Lilly and Company. Lilly is responsible for all clinical development and commercialization activities. LY2606368 is advancing in Phase 2 clinical trials for cancer. Prexasertib preferentially binds to and inhibits CHK1 and, to a lesser extent, inhibits CHK2. Chk-1 is a protein kinase that regulates the tumor cell's response to DNA damage often caused by treatment with chemotherapy. In response to DNA damage, Chk-1 blocks cell cycle progression in order to allow for repair of damaged DNA, thereby limiting the efficacy of chemotherapeutic agents. Inhibiting Chk-1 in combination with chemotherapy can enhance tumor cell death by preventing these cells from recovering from DNA damage.
PHA-793887 is an inhibitor of multiple cyclin dependent kinases (CDK) with activity against CDK2, CDK1 and CDK4. PHA-793887 was cytotoxic for leukemic cell lines in vitro, with IC(50) ranging from 0.3 to 7 uM. In colony assays PHA-793887 showed very high activity against leukemia cell lines, with an IC(50) <0.1 uM indicating that it has efficient and prolonged antiproliferative activity. PHA-793887 induced cell-cycle arrest, inhibited Rb and nucleophosmin phosphorylation. PHA-793887 has promising therapeutic activity against acute leukemias in vitro and in vivo.
Status:
Investigational
Source:
INN:morpheridine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Morpheridine is a pethidine analog with strong analgesic activity. Morpheridine does not cause convulsions, although it produces the standard opioid side effects such as sedation and respiratory depression. Morpheridine is not currently used in medicine and is a Schedule I drug which is controlled under United Nations drug conventions.
Status:
Investigational
Source:
INN:sardomozide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Sardomozide (previously known as SAM486A or CGP-48664) was developed as an inhibitor of S-adenosyl-methionine-decarboxylase, a key enzyme for polyamine biosynthesis. Sardomozide possessed the broad-spectrum antiproliferative and antitumor activity. The drug participated in a phase II clinical trial as a monotherapy in patients with refractory or relapsed non-Hodgkin's lymphoma. In Phase II clinical trial in patients with metastatic melanoma, the drug didn’t have significant therapeutic potential. The further development of this drug was discontinued.

Showing 4181 - 4190 of 4747 results