生物活性

• 描述Aromatic L-amino acid decarboxylase (AADC) is the final enzyme in the biosynthesis of the monoamine neurotransmitters serotonin and dopamine, and dopamine is the precursor for norepinephrine and epinephrine^[1]. Carbidopa monohydrate is the monohydrate form of Carbidopa. Carbidopa (CD), a competitive inhibitor of AADC that doesn't cross the blood-brain barrier, is routinely administered with levodopa (LD) to patients with Parkinson disease (PD) to reduce the peripheral decarboxylation of LD to dopamine^[2]. On exposure to other human tumor lines, CD was lethal only to NCI-H146 and NCI-H209 small cell lung carcinoma (SCLC) lines (IC₅₀ = 12 ± 1 μM and 22 ± 5 μM, respectively). CD (100 μM) decreased growth of SK-N-SH neuroblastoma and A204 rhabdomyosarcoma cells^[3]. For all patients with cerebrospinal fluid (CSF), AUC (area under the curve) serum CD significantly correlated with percent-labeled CSF HVA (R = 0.786, p = 0.02). In addition, a significantly greater percent-labeled CSF HVA was present in “rapid” as compared to “slow” CD absorbers (Patients were divided into “slow” absorbers (those unable to attain a serum CD level of at least 300 ng/ml within 3 hours after CD administration) and those with more “rapid” absorption (patients obtaining a level of 300 ng/ml or greater within the first 3 hours))^[2].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01754129	-	-	Completed	-	-
  NCT01754129	-	-	Completed	-	-
  NCT00357994	Advanced Parkinson's Disease	Phase 3	Completed	-	United States, California ... more >> Site Reference ID/Investigator# 45719 Los Angeles, California, United States, 90033 United States, Colorado Site Reference ID/Investigator# 45718 Englewood, Colorado, United States, 80113 United States, District of Columbia Site Reference ID/Investigator# 45722 Washington, District of Columbia, United States, 20007 United States, Florida Site Reference ID/Investigator# 45721 Bradenton, Florida, United States, 34205 Site Reference ID/Investigator# 45705 Gainesville, Florida, United States, 32610 United States, Maryland Site Reference ID/Investigator# 45740 Baltimore, Maryland, United States, 21201 United States, Missouri Site Reference ID/Investigator# 45739 St. Louis, Missouri, United States, 63110 United States, Vermont Site Reference ID/Investigator# 45703 Burlington, Vermont, United States, 05401 Germany Site Reference ID/Investigator# 44970 Bochum, Germany, 44791 Site Reference ID/Investigator# 44971 Bremerhaven, Germany, 27574 Site Reference ID/Investigator# 44973 Dresden, Germany, 01307 Site Reference ID/Investigator# 44965 Hanover, Germany, 30625 Site Reference ID/Investigator# 44964 Kiel, Germany, 24105 Site Reference ID/Investigator# 44966 Marburg, Germany, 35033 Site Reference ID/Investigator# 44968 Tuebingen, Germany, 72076 Collapse <<

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• 参考文献

• [1] Wassenberg T, Molero-Luis M, Jeltsch K, et al. Consensus guideline for the diagnosis and treatment of aromatic l-amino acid decarboxylase (AADC) deficiency. Orphanet J Rare Dis. 2017;12(1):12

  [2] Durso R, Evans JE, Josephs E, et al. Variable absorption of carbidopa affects both peripheral and central levodopa metabolism. J Clin Pharmacol. 2000;40(8):854‐860

  [3] Gilbert JA, Frederick LM, Ames MM. The aromatic-L-amino acid decarboxylase inhibitor carbidopa is selectively cytotoxic to human pulmonary carcinoid and small cell lung carcinoma cells. Clin Cancer Res. 2000;6(11):4365‐4372