Inxight Drugs

Showing 1 - 10 of 14 results

Status:

US Approved Rx (2003)

First approved in 1991

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Fludarabine or fludarabine phosphate is a chemotherapy drug used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas). It is a purine analog, which interferes with DNA synthesis. Fludarabine phosphat...

TAMOXIFEN

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094ZI81Y45

Status:

US Approved Rx (2003)

First approved in 1977

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Tamoxifen (brand name Nolvadex), is selective estrogen receptor modulators (SERM) with tissue-specific activities for the treatment and prevention of estrogen receptor positive breast cancer. Tamoxifen itself is a prodrug, having relatively little af...

finity for its target protein, the estrogen receptor (ER). It is metabolized in the liver by the cytochrome P450 isoform CYP2D6 and CYP3A4 into active metabolites such as 4-hydroxytamoxifen (4-OHT) (afimoxifene) and N-desmethyl-4-hydroxytamoxifen (endoxifen) which have 30–100 times more affinity with the ER than tamoxifen itself. These active metabolites compete with estrogen in the body for binding to the ER. In breast tissue, 4-OHT acts as an ER antagonist so that transcription of estrogen-responsive genes is inhibited. Tamoxifen has 7% and 6% of the affinity of estradiol for the ERα and ERβ, respectively, whereas 4-OHT has 178% and 338% of the affinity of estradiol for the ERα and ERβ. The prolonged binding of tamoxifen to the nuclear chromatin of these results in reduced DNA polymerase activity, impaired thymidine utilization, blockade of estradiol uptake, and decreased estrogen response. It is likely that tamoxifen interacts with other coactivators or corepressors in the tissue and binds with different estrogen receptors, ER-alpha or ER-beta, producing both estrogenic and antiestrogenic effects. Tamoxifen is currently used for the treatment of both early and advanced estrogen receptor (ER)-positive (ER+) breast cancer in pre- and post-menopausal women. Additionally, it is the most common hormone treatment for male breast cancer. Patients with variant forms of the gene CYP2D6 (also called simply 2D6) may not receive full benefit from tamoxifen because of too slow metabolism of the tamoxifen prodrug into its active metabolites. Tamoxifen is used as a research tool to trigger tissue-specific gene expression in many conditional expression constructs in genetically modified animals including a version of the Cre-Lox recombination technique. Tamoxifen has been shown to be effective in the treatment of mania in patients with bipolar disorder by blocking protein kinase C (PKC), an enzyme that regulates neuron activity in the brain. Researchers believe PKC is over-active during the mania in bipolar patients.

DOXORUBICIN

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80168379AG

Status:

US Approved Rx (2024)

First approved in 1974

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Development Status

Primary Target

Highest Phase

Approval Year

Condition

Treatment Modality

CNS Activity

Originator

Substance Class

Code System

ATC Level 1

ATC Level 2

ATC Level 3

ATC Level 4

Substance Form

FLUDARABINE

P2K93U8740

TAMOXIFEN

094ZI81Y45

DOXORUBICIN

80168379AG

FLUDARABINE PHOSPHATE

1X9VK9O1SC

TAMOXIFEN HYDROCHLORIDE

X545Q5UB3E

TAMOXIFEN CITRATE, (E)-

U7FJP95NF4

TAMOXIFEN CITRATE

7FRV7310N6

AVA-6000

7XPB9B6MUA

ZOPTARELIN DOXORUBICIN ACETATE

4IA03SIO30

ZOPTARELIN DOXORUBICIN

27844X2J29