Inxight Drugs

Showing 1 - 10 of 257 results

Status:

US Approved Rx (2018)

First approved in 2018

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Apalutamide (developmental code name ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment. Apalutamide binds to AR in target tissues thereby preventing androgen-induced receptor ...

OBETICHOLIC ACID

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0462Z4S4OZ

Status:

US Approved Rx (2016)

First approved in 2016

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Obeticholic acid (also known as INT-747), is a potent, orally bioavailable farnesoid X receptor (FXR) agonist. The key role of the farnesoid X receptor (FXR) as a regulator of bile and cholesterol metabolism in the liver, with preclinical data from n...

EDOXABAN

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NDU3J18APO

Status:

US Approved Rx (2015)

First approved in 2015

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Edoxaban (DU-176b, trade names Savaysa, Lixiana) is a selective factor Xa inhibitor reduces thrombin generation and thrombus formation and is an orally bioavailable anticoagulant drug. It was developed by Daiichi Sankyo to reduce the risk of stroke a...

OSIMERTINIB

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3C06JJ0Z2O

Status:

US Approved Rx (2015)

First approved in 2015

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Osimertinib is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug developed by AstraZeneca Pharmaceuticals. Its use is indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) in...

LENVATINIB

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EE083865G2

Status:

US Approved Rx (2022)

First approved in 2015

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Lenvatinib, developed by Eisai Co., is a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). Lenvatinib also inhibits othe...

IDELALISIB

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YG57I8T5M0

Status:

US Approved Rx (2014)

First approved in 2014

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Idelalisib is a first-in-class selective inhibitor of adenosine-5'-triphosphate (ATP) binding to PI3Kdelta kinase, resulting in inhibition of the P13K signalling pathway in malignant B cells. The compound is approved for the treatment of several typ...

PASIREOTIDE

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98H1T17066

Status:

US Approved Rx (2012)

First approved in 2012

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor, indicated for the treatment of adult patients with Cushing’s disease for whom pituitary surgery is not a...

COBICISTAT

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LW2E03M5PG

Status:

US Approved Rx (2015)

First approved in 2012

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Cobicistat (GS-9350) is a potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes. Cobicistat is a pharmacokinetic booster of several antiretrovirals. TYBOST (cobicistat) is indicated to increase systemic exposure of atazanavir or...

BENZNIDAZOLE

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YC42NRJ1ZD

Status:

US Approved Rx (2017)

First approved in 2011

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Benznidazole is an antiparasitic medication used in first-line treatment of Chagas disease. Benznidazole is a nitroimidazole antiparasitic with good activity against acute infection with Trypanosoma cruzi, commonly referred to as Chagas disease. Like...

other nitroimidazoles, benznidazole's main mechanism of action is to generate radical species which can damage the parasite's DNA or cellular machinery. Under anaerobic conditions, the nitro group of nitroimidazoles is believed to be reduced by the pyruvate:ferredoxin oxidoreductase complex to create a reactive nitro radical species. The nitro radical can then either engage in other redox reactions directly or spontaneously give rise to a nitrite ion and imidazole radical instead. In mammals, the principal mediators of electron transport are NAD+/NADH and NADP+/NADPH, which have a more positive reduction potential and so will not reduce nitroimidazoles to the radical form. This limits the spectrum of activity of nitroimidazoles so that host cells and DNA are not also damaged. This mechanism has been well-established for 5-nitroimidazoles such as metronidazole, but it is unclear if the same mechanism can be expanded to 2-nitroimidazoles (including benznidazole). In the presence of oxygen, by contrast, any radical nitro compounds produced will be rapidly oxidized by molecular oxygen, yielding the original nitroimidazole compound and a superoxide anion in a process known as "futile cycling". In these cases, the generation of superoxide is believed to give rise to other reactive oxygen species. The degree of toxicity or mutagenicity produced by these oxygen radicals depends on cells' ability to detoxify superoxide radicals and other reactive oxygen species. In mammals, these radicals can be converted safely to hydrogen peroxide, meaning benznidazole has very limited direct toxicity to human cells. In Trypanosoma species, however, there is a reduced capacity to detoxify these radicals, which results in damage to the parasite's cellular machinery. Benznidazole has a significant activity during the acute phase of Chagas disease, with a therapeutical success rate up to 80%. Its curative capabilities during the chronic phase are, however, limited. Some studies have found parasitologic cure (a complete elimination of T. cruzi from the body) in pediatric and young patients during the early stage of the chronic phase, but overall failure rate in chronically infected individuals is typically above 80%. However, some studies indicate treatment with benznidazole during the chronic phase, even if incapable of producing parasitologic cure, because it reduces electrocardiographic changes and a delays worsening of the clinical condition of the patient. Side effects tend to be common and occur more frequently with increased age. The most common adverse reactions associated with benznidazole are allergic dermatitis and peripheral neuropathy. It is reported that up to 30% of people will experience dermatitis when starting treatment. Benznidazole may cause photosensitization of the skin, resulting in rashes. Rashes usually appear within the first 2 weeks of treatment and resolve over time. In rare instances, skin hypersensitivity can result in exfoliative skin eruptions, edema, and fever. Peripheral neuropathy may occur later on in the treatment course and is dose-dependent. Other adverse reactions include anorexia, weight loss, nausea, vomiting, insomnia, and dyslexia, and bone marrow suppression. Gastrointestinal symptoms usually occur during the initial stages of treatment and resolves over time. Bone marrow suppression has been linked to the cumulative dose exposure.

VEMURAFENIB

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207SMY3FQT

Status:

US Approved Rx (2011)

First approved in 2011

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Vemurafenib (trade name Zelboraf) is a low molecular weight, orally available kinase inhibitor. It inhibits of some mutated forms of BRAF serinethreonine kinase, including BRAF V600E and is indicated for the treatment of patients with unresectable or...

Development Status

Primary Target

Highest Phase

Approval Year

Condition

Treatment Modality

CNS Activity

Originator

Substance Class

INN Stem

Code System

ATC Level 1

ATC Level 2

ATC Level 3

ATC Level 4

Substance Form

APALUTAMIDE

4T36H88UA7

OBETICHOLIC ACID

0462Z4S4OZ

EDOXABAN

NDU3J18APO

OSIMERTINIB

3C06JJ0Z2O

LENVATINIB

EE083865G2

IDELALISIB

YG57I8T5M0

PASIREOTIDE

98H1T17066

COBICISTAT

LW2E03M5PG

BENZNIDAZOLE

YC42NRJ1ZD

VEMURAFENIB

207SMY3FQT