Inxight Drugs

Showing 1 - 10 of 135 results

Status:

US Approved Rx (2015)

First approved in 2015

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Isavuconazole is an active form of isavuconazonium, a prodrug which is marketed under the name Cresemba. Isavuconazole inhibits lanosterol 14-alpha demethylase (or CYP51A1) and leads to the accumulation of ergosterol toxic precursors in the fungal cy...

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.

ORLISTAT

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95M8R751W8

Status:

US Approved Rx (2007)

First approved in 1999

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Orlistat or tetrahydrolipstatin (Xenical, Hoffmann-La Roche) is a saturated derivative of lipstatin originally isolated from Streptomyces toxytricini. Orlistat (Xenical, Hoffmann-La Roche) is a powerful inhibitor of gastrointestinal lipase and as suc...

5'-DEOXY-5-FLUOROCYTIDINE

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8RWB05I6ON

Status:

US Approved Rx (2018)

First approved in 1998

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Capecitabine is a fluoropyrimidine carbamate with antineoplastic activity. It is an orally administered systemic prodrug which is converted to 5-fluorouracil (5-FU). Both normal and tumor cells metabolize 5-FU to 5-fluoro-2’-deoxyuridine monophosphat...

ACITRETIN

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LCH760E9T7

Status:

US Approved Rx (2024)

First approved in 1996

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Acitretin is all-Trans-9-(4-methoxy-2, 3, 6¬ trimethylphenyl)-three, 7-dimethyl-2, 4, 6, 8-nonatetraenoic acid. It is a metabolite of exterminate and is related to both retinoic acid and retinol (vitamin A). It is taken orally, and is typically used ...

CEFTRIAXONE

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75J73V1629

Status:

US Approved Rx (2006)

First approved in 1984

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Ceftriaxone is a broad-spectrum cephalosporin antibiotic with a very long half-life. Ceftriaxone is a bactericidal agent that acts by inhibition of bacterial cell wall synthesis. Ceftriaxone has activity in the presence of some beta-lactamases, both ...

CYCLOBENZAPRINE

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69O5WQQ5TI

Status:

US Approved Rx (1995)

First approved in 1977

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Cyclobenzaprine is a centrally-acting muscle relaxant which boosts levels of norepinephrine and binds to serotonin receptors in the brain to reduce spasm. Cytochromes P-450 3A4, 1A2, and, to a lesser extent, 2D6, mediate N-demethylation, one of the o...

FLUCYTOSINE

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D83282DT06

Status:

US Approved Rx (1971)

First approved in 1971

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Flucytosine (5-flucytosine, Ancobon) is an antifungal agent used for treatment of serious fungal infections caused by Candida or Cryptococcus. A fluorinated cytosine analog it was originally developed as an anti-tumor agent, but was found to be non-e...

LEVODOPA

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46627O600J

Status:

US Approved Rx (2019)

First approved in 1970

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Levodopa (L-DOPA) was first isolated from seedlings of Vicia faba by Marcus Guggenheim in 1913. Levodopa, a dopamine precursor, is an effective and well-tolerated dopamine replacement agent used to treat Parkinson's disease. Oral levodopa has been wi...

NORTRIPTYLINE

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BL03SY4LXB

Status:

US Approved Rx (1992)

First approved in 1964

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Nortriptyline is a second-generation tricyclic antidepressant (TCA) marketed as the hydrochloride salt under the trade names Sensoval, Aventyl, Pamelor, Norpress, Allegron, Noritren and Nortrilen. Nortriptyline is used in the treatment of depression ...

Originator

Development Status

Primary Target

Highest Phase

Approval Year

Condition

Treatment Modality

CNS Activity

Substance Class

Code System

ATC Level 1

ATC Level 2

ATC Level 3

ATC Level 4

Substance Form

Isavuconazole

60UTO373KE

BENZNIDAZOLE

YC42NRJ1ZD

ORLISTAT

95M8R751W8

5'-DEOXY-5-FLUOROCYTIDINE

8RWB05I6ON

ACITRETIN

LCH760E9T7

CEFTRIAXONE

75J73V1629

CYCLOBENZAPRINE

69O5WQQ5TI

FLUCYTOSINE

D83282DT06

LEVODOPA

46627O600J

NORTRIPTYLINE

BL03SY4LXB