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Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.
Status:
US Approved Allergenic Extract
(1994)
Source:
BLA103738
(1994)
Source URL:
First approved in 1994
Source:
BLA103738
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Quaternium-15, a preservative, is one of the most used substances and is added to several cosmetics and other industrial products. Quaternium-15 is a mixture of
isomers, where the cis-form is the dominant form and where the trans-form is the minor
component present as an impurity.
Quaternium-15 can be found under a variety of names, most commonly those of the Dow Chemical Company: Dowicil 200 (cis isomer only), Dowicil 75 and Dowicil 100 (both a mix of cis and trans isomers). The isolated cis-compound is used primarily in cosmetic applications, with a maximum permitted concentration in the EU of 0.2%. DOWICIL 200 preservative (cis form) is used primarily as a preservative in a wide variety of personal-care
and cosmetic products. It is designed to provide highly effective broad-spectrum antimicrobial
activity, especially in water-based formulations. It is used in both leave-on and rinse-off
application such as baby-care products, hair-care products, lotions, powders, and creams.
The mixed product (cis- and trans-) is used in a wider range of formulations such as: emulsifiable metal-cutting fluids; latex and emulsion paints; liquid floor polishes and floor waxes; glues and adhesives. Recently, the cis-form has been classified as a CMR substance with the classification
toxic to reproduction, category 3. This classification only concerns the cis-isomer:
Status:
US Approved Allergenic Extract
(1994)
Source:
BLA103738
(1994)
Source URL:
First approved in 1994
Source:
BLA103738
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Clove oil is a natural product, derived from the Eugenia caryophyllata tree. Clove oil is 85 to 95% eugenol. Isoeugenol and methyleugenol make up 5 to 15% of the remaining ingredients. Isoeugenol is manufactured from eugenol by a process of isomerization. Isoeugenol have been used in foods and eugenol has been used in animal feeds. Isoeugenol is used as a fish anesthetic. The mechanism of action of isoeugenol in fish has not been determined. It is hypothesised that its effects are mediated via receptors controlling cellular ion channels in a similar way to that described for local anaesthetics. Reports of adverse reactions involving the use of isoeugenol in humans are primarily confined to incidents of contact sensitization or allergy following dermal exposure.
Status:
US Approved Allergenic Extract
(1994)
Source:
BLA103738
(1994)
Source URL:
First approved in 1994
Source:
BLA103738
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Quaternium-15, a preservative, is one of the most used substances and is added to several cosmetics and other industrial products. Quaternium-15 is a mixture of
isomers, where the cis-form is the dominant form and where the trans-form is the minor
component present as an impurity.
Quaternium-15 can be found under a variety of names, most commonly those of the Dow Chemical Company: Dowicil 200 (cis isomer only), Dowicil 75 and Dowicil 100 (both a mix of cis and trans isomers). The isolated cis-compound is used primarily in cosmetic applications, with a maximum permitted concentration in the EU of 0.2%. DOWICIL 200 preservative (cis form) is used primarily as a preservative in a wide variety of personal-care
and cosmetic products. It is designed to provide highly effective broad-spectrum antimicrobial
activity, especially in water-based formulations. It is used in both leave-on and rinse-off
application such as baby-care products, hair-care products, lotions, powders, and creams.
The mixed product (cis- and trans-) is used in a wider range of formulations such as: emulsifiable metal-cutting fluids; latex and emulsion paints; liquid floor polishes and floor waxes; glues and adhesives. Recently, the cis-form has been classified as a CMR substance with the classification
toxic to reproduction, category 3. This classification only concerns the cis-isomer:
Status:
US Approved Allergenic Extract
(1994)
Source:
BLA103738
(1994)
Source URL:
First approved in 1961
Source:
NDA012911
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Propylparaben is a bacteriostatic and fungistatic agent used as a preservative in cosmetic products, food and drugs. As a food additive, it has the E number E216. To increase the activity and reduce its dose propylparaben is used in a mixture with other parabens and in combination with other types of preservatives. Propylparaben is a chemical allergen capable of producing immunologically mediated hypersensitivity reactions. Chemically it is an ester of p-hydroxybenzoic acid.
Status:
US Previously Marketed
Source:
OMLONTI by OCUVEX THERAP
(2022)
Source URL:
First approved in 2022
Source:
OMLONTI by OCUVEX THERAP
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Omidenepag isopropyl, a prodrug, is hydrolyzed in the eye to the active form (Omidenepag) which functions as a selective, nonprostaglandin, prostanoid EP2 agonist, has been developed by Ube Industries and Santen Pharmaceutical as an ophthalmic solution (EYBELIS®) for the treatment of glaucoma and ocular hypertension. Omidenepag isopropyl increases the outfow of aqueous humor via both the uveoscleral outfow and the trabecular outfow pathways, resulting in potent and stable reduction in intraocular pressure (IOP). In September 2018, omidenepag isopropyl ophthalmic solution 0.002% was approved in Japan for the treatment of glaucoma and ocular hypertension. On September 22, 2022, the FDA approved Santen’s Omlonti (omidenepag isopropyl), for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
Status:
US Previously Marketed
Source:
EXKIVITY by TAKEDA PHARMS USA
(2021)
Source URL:
First approved in 2021
Source:
EXKIVITY by TAKEDA PHARMS USA
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Mobocertinib (EXKIVITY™) is a first-in-class EGFR tyrosine kinase inhibitor being developed for the treatment of EGFR exon 20 insertion (EGFRex20ins) -positive non-small cell lung cancer (NSCLC). Mobocertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR) that irreversibly binds to and inhibits EGFR exon 20 insertion mutations at lower concentrations than wild type (WT) EGFR. Two pharmacologically-active metabolites (AP32960 and AP32914) with similar inhibitory
profiles to mobocertinib have been identified in the plasma after oral administration of mobocertinib. In vitro, mobocertinib also inhibited the activity of other EGFR family members (HER2 and HER4) and one additional kinase (BLK) at clinically relevant concentrations (IC50 values <2 nM). Based on efficacy in patients whose disease had progressed on or after platinum-based therapy in a phase I/II trial, mobocertinib was recently granted accelerated approval in the USA in this indication. The drug is also being assessed for marketing approval in various other countries and territories including the EU and China.
Status:
US Previously Marketed
Source:
UKONIQ by TG THERAPS
(2021)
Source URL:
First approved in 2021
Source:
UKONIQ by TG THERAPS
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Umbralisib (Ukoniq, TG Therapeutics) is an orally available PI3K delta inhibitor, targeting the delta isoform with nanomolar potency and several fold selectivity over the alpha, beta, and gamma isoforms of PI3K. The delta isoform of PI3K is strongly expressed in cells of hematopoietic origin and is believed to be important in the proliferation and survival of B-cell lymphocytes. On February 5, 2021, the Food and Drug Administration granted accelerated approval to umbralisib for the following indications: adult patients with relapsed or refractory marginal zone lymphoma (MZL) who have received at least one prior anti-CD20-based regimen; adult patients with relapsed or refractory follicular lymphoma (FL) who have received at least three prior lines of systemic therapy. However, on June 1, 2022, the FDA withdrew its approval for the cancer medicine Ukoniq due to safety concerns.
Status:
US Previously Marketed
Source:
BEVYXXA by PORTOLA PHARMS INC
(2017)
Source URL:
First approved in 2017
Source:
BEVYXXA by PORTOLA PHARMS INC
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Betrixaban is an anticoagulant drug which acts as a direct factor Xa inhibitor. Betrixaban is now being developed by Portola Pharmaceuticals. Oral, once-daily Factor Xa inhibitor anticoagulant that directly inhibits the activity of Factor Xa, an important validated target in the blood coagulation pathway, to prevent life-threatening thrombosis. U.S. Food and Drug Administration granted Fast Track designation to betrixaban for extended-duration prevention of venous thromboembolism (VTE; blood clots) in acute medically ill patients (i.e., those who are hospitalized for serious medical conditions, such as heart failure, stroke, infection and pulmonary disease). Has the potential to become the first oral Factor Xa inhibitor anticoagulant approved for hospital-to-home prevention of VTE in acute medically ill patients.
Status:
US Previously Marketed
Source:
ALIQOPA by BAYER HEALTHCARE
(2017)
Source URL:
First approved in 2017
Source:
ALIQOPA by BAYER HEALTHCARE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Copanlisib, developed by Bayer, is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Copanlisib inhibits the activation of the PI3K signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. Copanlisib is currently under Phase II/III clinical trials for the treatment of non-Hodgkin lymphoma and chronic lymphocytic leukemia.