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Restrict the search for
penicillin g
to a specific field?
Status:
US Approved Rx
(2018)
Source:
NDA210496
(2018)
Source URL:
First approved in 2018
Source:
NDA210496
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Encorafenib, also known as BRAFTOVI or LGX818, is an orally available mutated BRaf V600E inhibitor with potential antineoplastic activity, which was developed by Novartis. LGX818 possesses selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E. In the A375 (BRAFV600E) human melanoma cell line LGX818 suppresses phospho-ERK (EC50 = 3 nM) leading to potent inhibition of proliferation (EC50 = 4 nM). No significant activity was observed against a panel of 100 kinases (IC50 > 900 nM) and LGX818 did not inhibit proliferation of > 400 cell lines expressing wild-type BRAF. On June 27, 2018, the Food and Drug Administration approved encorafenib and Binimetinib (BRAFTOVI and MEKTOVI, Array BioPharma Inc.) in combination for patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test. Encorafenib and binimetinib target two different kinases in the RAS/RAF/MEK/ERK pathway. Compared with either drug alone, co-administration of encorafenib and binimetinib result in greater anti-proliferative activity in vitro in BRAF mutation-positive cell lines and greater anti-tumor activity with respect to tumor growth inhibition in BRAF V600E mutant human melanoma xenograft studies in mice. In addition to the above, the combination of encorafenib and binimetinib acted to delay the emergence of resistance in BRAF V600E mutant human melanoma xenografts in mice compared with the administration of either drug alone. Encorafenib is in phase III for Metastatic Colorectal Cancer and in phase II for Relapsed or Refractory Multiple Myeloma.
Status:
US Approved Rx
(2018)
Source:
NDA208700
(2018)
Source URL:
First approved in 2018
Source:
NDA208700
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Lutetium Lu 177 dotatate binds to somatostatin receptors with highest affinity for subtype 2 receptors (SSRT2). Upon binding to somatostatin
receptor expressing cells, including malignant somatostatin receptor-positive tumors, the compound is internalized. The beta emission from Lu 177
induces cellular damage by formation of free radicals in somatostatin receptor-positive cells and in neighboring cells. LUTATHERA® (lutetium Lu 177 dotatate) is indicated for the treatment of somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs), including foregut, midgut, and hindgut neuroendocrine tumors in adults.
Status:
US Approved Rx
(2018)
Source:
NDA209521
(2018)
Source URL:
First approved in 2018
Source:
NDA209521
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Sarecycline (SC1401, WC3035) is a novel, once-daily, tetracycline-derived compound being developed by Paratek Pharmaceuticals and Allergan (previously Actavis) for use in the treatment of acne and rosacea. In preclinical studies, Sarecycline possesses favorable anti-inflammatory activity, plus narrow-spectrum antibacterial activity relative to other tetracycline-derived molecules. Sarecycline has been used in Phase III clinical trials studying the treatment of Acne Vulgaris. The primary objective was to evaluate the efficacy and safety of oral Sarecycline 1.5 mg/kg per day compared to placebo in treating inflammatory acne lesions in subjects with moderate to severe acne. Sarecycline was statistically significantly superior to placebo with respect to primary efficacy endpoints. The most common adverse events (>2%) reported in the sarecycline group were nausea (3.2%), nasopharyngitis (2.8%), and headache (2.8%). The rate of discontinuation due to adverse events among sarecycline-treated patients in the two studies combined was 1.4%.
Status:
US Approved Rx
(2018)
Source:
NDA210951
(2018)
Source URL:
First approved in 2018
Source:
NDA210951
Source URL:
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 activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells. Apalutamide is currently in phase III clinical trials for castration-resistant prostate cancer.
Status:
US Approved Rx
(2018)
Source:
NDA211349
(2018)
Source URL:
First approved in 2018
Source:
NDA211349
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Gilteritinib, also known as ASP2215, is a potent FLT3/AXL inhibitor, which showed potent antileukemic activity against AML with either or both FLT3-ITD and FLT3-D835 mutations. In in vitro, among the 78 tyrosine kinases tested, Gilteritinib inhibited FLT3, LTK, ALK, and AXL kinases by over 50% at 1 nM with an IC50 value of 0.29 nM for FLT3, approximately 800-fold more potent than for c-KIT, the inhibition of which is linked to a potential risk of myelosuppression. Gilteritinib inhibited the growth of MV4-11 cells, which harbor FLT3-ITD, with an IC50 value of 0.92 nM, accompanied with inhibition of pFLT3, pAKT, pSTAT5, pERK, and pS6. Gilteritinib decreased tumor burden in bone marrow and prolonged the survival of mice intravenously transplanted with MV4-11 cells. In previous preclinical studies, gilteritinib has demonstrated superior antitumor effects when given in combination with AraC and either DNR or IDR compared with combination chemotherapy. In November 2018, the FDA approved gilteritinib for treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation as detected by an FDA-approved test.
Status:
US Approved Rx
(2018)
Source:
NDA211109
(2018)
Source URL:
First approved in 2018
Source:
NDA211109
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Eravacycline, known as Xerava by Tetraphase Pharmaceuticals, is a fully synthetic fluorocycline antibiotic of the tetracycline class with activity against clinically significant gram-negative, gram-positive aerobic, and facultative bacteria. This includes most of those bacteria resistant to cephalosporins, fluoroquinolones, β-lactam/β-lactamase inhibitors, multidrug-resistant strains, and carbapenem-resistant Enterobacteriaceae, and the majority of anaerobic pathogens. It was first approved by the FDA on August 27, 2018. Eravacycline disrupts bacterial protein synthesis by binding to the 30S ribosomal subunit thus preventing the incorporation of amino acid residues into elongating peptide chains.
Status:
US Approved Rx
(2018)
Source:
NDA211155
(2018)
Source URL:
First approved in 2018
Source:
NDA211155
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Duvelisib (IPI-145), is an orally available, small-molecule, selective dual inhibitor of phosphatidylinositol 3 kinase (PI3K) δ and γ isoforms originated by Intellikine (owned by Takeda) and developed by Infinity Pharmaceuticals. Orally administered duvelisib was rapidly absorbed, with a dose-proportional increase in exposure. The compound produced a half-life of approximately 7-12 hours, following 14 days of dosing. Duvelisib exerts profound effects on adaptive and innate immunity by inhibiting B and T cell proliferation, blocking neutrophil migration, and inhibiting basophil activation. Duvelisib blockade of PI3K-δ and PI3K-γ potentially lead to significant therapeutic effects in multiple inflammatory, autoimmune, and hematologic diseases. The molecule is in phase III development as a combination therapy for patients with haematological malignancies such as chronic lymphocytic leukemia and follicular lymphoma.
Status:
US Approved Rx
(2018)
Source:
NDA210303
(2018)
Source URL:
First approved in 2018
Source:
NDA210303
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Plazomicin is a novel aminoglycoside antibiotic that binds to the bacterial 30S ribosomal subunit, thus inhibiting protein synthesis in a concentration-dependent manner. Plazomicin displays a broad spectrum of activity against aerobic gram-negative bacteria including extended-spectrum β-lactamase-producing Enterobacteriaceae, carbapenem-resistant Enterobacteriaceae, and organisms with aminoglycoside-modifying enzymes. Plazomicin resistance in Enterobacteriaceae is via modification of the ribosomal binding site due to expression of 16S rRNA methyltransferases. ZEMDRI (plazomicin) injection for intravenous use is indicated for the treatment of patients 18 years of age or older with Complicated Urinary Tract Infections (cUTI) including Pyelonephritis.
Status:
US Approved Rx
(2018)
Source:
NDA206709
(2018)
Source URL:
First approved in 2018
Source:
NDA206709
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Stiripentol is an anticonvulsant drug used in the treatment of epilepsy. It recently proved to increase the GABAergic transmission in vitro in an experimental model of immature rat. Clinical studies were based on the fact that STP also acts as an inhibitor of CYP3A4, CYP1A2, and CYP2C19 in vivo in epileptic patients. Side effects are largely due to the increase in plasma concentrations of other anticonvulsants and can be reduced by lowering the dose of those drugs. Nausea and vomiting are particularly noted when used in combination with sodium valproate. It appears to increase the potency of phenobarbital, primidone, phenytoin, carbamazepine, clobazam and diazepam.
Status:
US Approved Rx
(2019)
Source:
NDA209569
(2019)
Source URL:
First approved in 2018
Source:
21 CFR 348
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Brilliant Blue G is triphenylmethane dye that was developed for use in the textile industry but is now commonly used for staining proteins in analytical biochemistry. The Bradford assay is a standard, rapid dye-binding assay that uses Brilliant Blue G to quantify the amount of protein in a solution. Brilliant Blue G also acts as a selective inhibitor of the P2X purinoceptor channel P2X7 (IC50s = 10.1 and 265 nM for rat and human P2X7, respectively). In mice, it inhibits interleukin-1β expression and reduces neurological injury secondary to traumatic brain injury. Brilliant Blue G was used to prepare the protein reagent for the determination of protein content of the collagenase enzyme isolated from fish waste. It may be employed as a stain for the internal limiting membrane (ILM) for the macular hole (MH) and epiretinal membrane (ERM) surgery.
