Inxight Drugs

Showing 1 - 10 of 111 results

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...

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...

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.

DEGARELIX

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SX0XJI3A11

Status:

US Approved Rx (2008)

First approved in 2008

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

DEGARELIX (FIRMAGON®) is a synthetic linear decapeptide amide containing seven unnatural amino acids, five of which are D-amino acids. It is a GnRH receptor antagonist. It binds reversibly to the pituitary GnRH receptors, thereby reducing the release...

AMBRISENTAN, (±)-

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7B43003091

Status:

US Approved Rx (2022)

First approved in 2007

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Conditions:

Ambrisentan (alternative Names: BSF 208075; GSK 1325760; GSK1325760A; Letairis) is an endothelin receptor antagonist that is selective for the endothelin type-A (ETA) receptor. The chemical name of ambrisentan is (+)-(2S)-2-[(4,6-dimethylpyrimidin-2-...

NILOTINIB

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F41401512X

Status:

US Approved Rx (2007)

First approved in 2007

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Nilotinib (AMN107, trade name Tasigna) is a kinase inhibitor indicated for the treatment of chronic phase and accelerated phase Philadelphia chromosome-positive chronic myelogenous leukemia (CML) in adult patients resistant to or intolerant to prior ...

RIFAPENTINE

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XJM390A33U

Status:

US Approved Rx (1998)

First approved in 1998

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

PRIFTIN® (rifapentine) is indicated in adults and children 12 years and older for the treatment of active pulmonary tuberculosis (TB) caused by Mycobacterium tuberculosis. PRIFTIN must always be used in combination with one or more antituberculosis (...

VENLAFAXINE

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GRZ5RCB1QG

Status:

US Approved Rx (2018)

First approved in 1993

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Conditions:

Venlafaxine is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor, which is sold under several brand names; one of them is venlafaxine hydrochloride. Venlafaxine hydrochloride is a venlafaxine extended release tablets, which are indicate...

RIFABUTIN

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1W306TDA6S

Status:

US Approved Rx (2019)

First approved in 1992

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Rifabutin is an antibiotic that inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme. It is bactericidal and has a very broad spectrum ...

ATOVAQUONE

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Y883P1Z2LT

Status:

US Approved Rx (2011)

First approved in 1992

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Atovaquone is a chemical compound that belongs to the class of naphthoquinones; it is manufactured in the US in the liquid form, or oral suspension, under the brand name Mepron. Meron is used for the treatment or prevention of Pneumocystis carinii pn...

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

OBETICHOLIC ACID

0462Z4S4OZ

PASIREOTIDE

98H1T17066

BENZNIDAZOLE

YC42NRJ1ZD

DEGARELIX

SX0XJI3A11

AMBRISENTAN, (±)-

7B43003091

NILOTINIB

F41401512X

RIFAPENTINE

XJM390A33U

VENLAFAXINE

GRZ5RCB1QG

RIFABUTIN

1W306TDA6S

ATOVAQUONE

Y883P1Z2LT