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Labetuzumab govitecan
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DB12331 |
[Labetuzumab govitecan has been used in trials studying the treatment of Colon Cancer, Rectal Cancer, and Metastatic Colorectal Cancer.] |
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Rucaparib
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DB12332 |
[Rucaparib is a potent mammalian poly(ADP-ribose) polymerase (PARP) 1, 2 and 3 inhibitor with anticancer properties. PPAR is an enzyme that plays an essential role in DNA repair by activating response pathways and facilitating repair [A18745], and defects in these repair mechanisms have been demonstrated in various malignancies, including cancer. Regulation of repair pathways is critical in promoting necessary cell death. BRCA genes are tumor suppressor genes mediate several cellular process including DNA replication, transcription regulation, cell cycle checkpoints, apoptosis, chromatin structuring and homologous recombination (HR). Homologous recombination deficiency (HRD), along with PPAR inhibition, is a vulnerability that enhances the cell death pathway when the single mutations alone would permit viability. Ovarian cancer commonly possesses defects in DNA repair pathways such as HRD due to BRCA mutations or otherwise.
There are three main types of ovarian cancer: epithelial (90%), germ cell (5%) and sex cord stromal cell (5%). Epithelial ovarian, being the most common, fifth leading cause of cancer-related deaths in women in the United States. Advanced ovarian cancer particularly poses challenges due to reduced therapeutic response rates from standard platinum-based chemotherapy and overall survival rates. Rucaparib has shown to induce cytotoxicity in tumor cell lines with deficiencies in BRCA1/2 and other DNA repair genes [FDA Label]. Of all the BRCA1/2 mutations in ovarian cancer, most are due to germline mutations (18%), and approximately 7% represent somatic mutations acquired within the tumor [A31354].
The indication of rucaparib as an oral monotherapy in patients with deleterious BRCA mutation (germline and/or somatic) associated advanced ovarian cancer was granted accelerated approval in 2016 for selected patients who have previously received greater than two lines of platinum-based therapy. It is currently marketed in the US under the brand name Rubraca that contains rucaparib camsylate as the active ingredient. The identification of patients who are eligible for rucaparib therapy is performed via *in vitro* diagnostic tests to detect the presence of a deleterious BRCA mutation (germline and/or somatic). The FDA-approved test qualitatively detects sequence alterations in BRCA1 and BRCA2 (BRCA1/2) genes. More information can be found on the FDA Website [L1047].
While rucaparib is indicated for deleterious BRCA mutation (germline and/or somatic)-associated advanced ovarian cancer, there is evidence that its antitumor activity is also clinically effective against ovarian tumors with high homologous recombination deficiency (HRD) loss of heterozygosity (LOH) [A31354].] |
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Clofenamide
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DB13663 |
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Pyrotinib
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DB14993 |
[Pyrotinib is under investigation in clinical trial NCT03756064 (Neoadjuvant Study of Pyrotinib in Patients With HER2 Positive Breast Cancer).] |
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Influenza B virus B/Utah/9/2014 antigen (MDCK cell derived, propiolactone inactivated)
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DB11002 |
[A seasonally-specific component of the influenza vaccine. The influenza vaccine, also known as the "flu shot", is a vaccine that protects against infection from the influenza viruses. Vaccines provide protection from influenza by exposing the immune system to the virus (or parts of the virus) which stimulates an immunological defence against future exposure to the virus, or "antigen". This defence includes the production of humoral immunity through the development of antibodies (through memory B cells) and of cell-mediated immunity through the production of T-lymphocytes. Upon re-exposure to infectious influenza virus, the immune system is prepared to identify and destroy the virus as there are circulating antibodies that recognize that particular component of the virus that it was previously exposed to.
There are two basic types of vaccines available: inactivated influenza vaccine (IIV) and live attenuated influenza vaccine (LAIV). Inactivated vaccines contain a virus particle that has been grown in media and then subsequently killed, or inactivated, through exposure to heat or chemicals such as formaldehyde 3. Inactivated virus cannot replicate, and therefore cannot cause disease from infection, even in immunocompromised individuals. In contrast, live vaccines are produced from "wild-type" or disease-causing viruses that have been attenuated, or weakened, through various laboratory techniques. Live vaccines maintain their replicative ability.] |
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Bazlitoran
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DB14990 |
[Bazlitoran is under investigation in clinical trial NCT02092909 (Phase 1/2 Dose Escalation Study in Patients With Relapsed or Refractory Waldenstrom's Macroglobulinemia).] |
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Sulfadiazine
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DB00359 |
[One of the short-acting sulfonamides used in combination with pyrimethamine to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.] |
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Mefloquine
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DB00358 |
[A phospholipid-interacting antimalarial drug (antimalarials). It is very effective against plasmodium falciparum with very few side effects. [PubChem]] |
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Inhibitor Idd 384
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DB01689 |
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Aztreonam
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DB00355 |
[A monocyclic beta-lactam antibiotic originally isolated from Chromobacterium violaceum. It is resistant to beta-lactamases and is used in gram-negative infections, especially of the meninges, bladder, and kidneys. It may cause a superinfection with gram-positive organisms.] |
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N,N-dimethylarginine
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DB01686 |
[Asymmetric dimethylarginine (ADMA) is a naturally occurring chemical found in blood plasma. It is a metabolic by-product of continual protein modification processes in the cytoplasm of all human cells which is closely related to L-arginine, a conditionally-essential amino acid. ADMA interferes with L-arginine in the production of nitric oxide, a key chemical to endothelial and hence cardiovascular health.] |
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Buclizine
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DB00354 |
[Buclizine is an antihistamine medication with both antiemetic and anticholinergic effects [L6220], belonging to the _piperazine derivative_ family of drugs. It was manufactured by Stuart Pharms and initially approved by the FDA in 1957.[L6217] Following this, it was touted to be effective as an appetite stimulant in children when administered in the syrup form, however, this indication has not been validated.[A178102] In addition to the above conditions, buclizine has been studied in the treatment of migraine attacks and in the treatment of nausea and vomiting during pregnancy. [A178105, A178108]] |
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Topiroxostat
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DB01685 |
[Topiroxostat is a selective xanthine oxidase inhibitor developed for treatment and management of hyperuricemia and gout. Xanthine oxidase, or xanthine oxidoreductase (XOR), regulates purine metabolism, and inhibition of the enzyme results in efficacious reduction of serum urate levels. Xanthine oxidase inhibitors are classified into two groups; purine analogs such as [DB00437] and [DB05262], and non-purine agents which includes topiroxostat. While [DB00437] is considered a first-line therapy in treating hyperuricemic conditions, it is often associated with side effects and ineffective in reducing uric acid levels under recommended dosing regimens. Renal complications are major comorbidities that limit the [DB00437] therapy as dose reductions are recommended. Topiroxostat and its metabolites are shown to be unaffected by renal complications, thus may be effective in patients with chronic kidney diseases [A19657]. Approved for therapeutic use in Japan since 2013, topiroxostat is marketed under the name Topiloric and Uriadec and is orally administered twice daily.] |
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Aminoglutethimide
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DB00357 |
[An aromatase inhibitor that produces a state of "medical" adrenalectomy by blocking the production of adrenal steroids. It also blocks the conversion of androgens to estrogens. Aminoglutethimide has been used in the treatment of advanced breast and prostate cancer. It was formerly used for its weak anticonvulsant properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p454)] |
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P-Cresol
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DB01688 |
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beta-Mannobiose
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DB01687 |
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Chlorzoxazone
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DB00356 |
[A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202)] |
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Megestrol acetate
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DB00351 |
[17-Hydroxy-6-methylpregna-3,6-diene-3,20-dione. A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer.] |
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6'-Methyl-Thiamin Diphosphate
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DB01682 |
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Benzene Hexacarboxylic Acid
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DB01681 |
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