Drug Information

Drug (ID: DG00268) and It's Reported Resistant Information

• Name: Calcitriol
• Synonyms: Calcitriol; Rocaltrol; 32222-06-3; Calcijex; Topitriol; 1alpha,25-Dihydroxyvitamin D3; Silkis; Soltriol; 1alpha,25-Dihydroxycholecalciferol; Calcitriolum; Dihydroxyvitamin D3; 1,25-DHCC; 1,25-Dihydroxyvitamin D; Vectical; 1,25-DIHYDROXYCHOLECALCIFEROL; 1,25-Dihydroxyvitamin D3; 1alpha,25-Dihydroxyvitamin D; 1-alpha,25-Dihydroxyvitamin D3; Calcitriolum [INN-Latin]; UNII-FXC9231JVH; 1alpha,25(OH)2D3; DN-101; 1,25-Dihydroxycholecaliferol; CCRIS 5522; Ro 21-5535; HSDB 3482; 1-alpha,25-Dihydroxycholecalciferol; EINECS 250-963-8; DN 101; Calcitriol (chemotherapy-induced alopecia); Calcitriol (chemotherapy-induced alopecia), Cytotech Labs; Calcitriol (API-31543, drug-induced alopecia), Cytotech Labs; 1alpha,25 dihydroxyvitamin D(3)
• Indication:
  In total 1 Indication(s)
  Hair/hair growth developmental defect [ICD-11: LC30]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Colon cancer [ICD-11: 2B90]; [1]
• Target: Vitamin D3 receptor (VDR); VDR_HUMAN; [1]
• Formula: C27H44O3
• IsoSMILES: C[C@H](CCCC(C)(C)O)[C@H]1CC[C@@H]\\2[C@@]1(CCC/C2=C\\C=C/3\\C[C@H](C[C@@H](C3=C)O)O)C
• InChI: 1S/C27H44O3/c1-18(8-6-14-26(3,4)30)23-12-13-24-20(9-7-15-27(23,24)5)10-11-21-16-22(28)17-25(29)19(21)2/h10-11,18,22-25,28-30H,2,6-9,12-17H2,1,3-5H3/b20-10+,21-11-/t18-,22-,23-,24+,25+,27-/m1/s1
• InChIKey: GMRQFYUYWCNGIN-NKMMMXOESA-N
• PubChem CID: 5280453
• ChEBI ID: CHEBI:17823
• TTD Drug ID: D0T2PL
• INTEDE ID: DR0260
• DrugBank ID: DB00136

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Colon cancer [ICD-11: 2B90]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: H19, imprinted maternally expressed transcript (H19) [1]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Colon cancer [ICD-11: 2B90.1]
• Experimental Note: Identified from the Human Clinical Data
• Cell Pathway Regulation: Wnt/Beta-catenin signaling pathway; Inhibition; hsa04310
• In Vitro Model: DLD1 cells; Colon; Homo sapiens (Human); CVCL_0248
• In Vitro Model: HT-29 cells; Colon; Homo sapiens (Human); CVCL_0320
• In Vivo Model: Nude mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: qRT-PCR
• Experiment for Drug Resistance: MTT assay
• Mechanism Description: H19 overexpression induces resistance to 1,25(OH)2D3 by inhibiting the expression of VDR Through miR675-5p in colon cancer cells. vdr signaling was able to attenuate the proliferation and migration of colon cancer cells via multiple mechanisms including inhibiting Wnt/beta-catenin pathway, VDR signaling inhibits the expression of h19 by regulating the C-Myc/mad-1 Network.

Key Molecule: hsa-miR-675-5p [1]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Colon cancer [ICD-11: 2B90.1]
• Experimental Note: Identified from the Human Clinical Data
• Cell Pathway Regulation: Wnt/Beta-catenin signaling pathway; Inhibition; hsa04310
• In Vitro Model: DLD1 cells; Colon; Homo sapiens (Human); CVCL_0248
• In Vitro Model: HT-29 cells; Colon; Homo sapiens (Human); CVCL_0320
• In Vivo Model: Nude mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: qRT-PCR
• Experiment for Drug Resistance: MTT assay
• Mechanism Description: H19 overexpression induces resistance to 1,25(OH)2D3 by inhibiting the expression of VDR Through miR675-5p in colon cancer cells. vdr signaling was able to attenuate the proliferation and migration of colon cancer cells via multiple mechanisms including inhibiting Wnt/beta-catenin pathway, VDR signaling inhibits the expression of h19 by regulating the C-Myc/mad-1 Network.

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Vitamin D3 receptor (VDR) [1]

• Molecule Alteration: Expression; Down-regulation
• Resistant Disease: Colon cancer [ICD-11: 2B90.1]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: DLD1 cells; Colon; Homo sapiens (Human); CVCL_0248
• In Vitro Model: HT-29 cells; Colon; Homo sapiens (Human); CVCL_0320
• In Vivo Model: Nude mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: RT-qPCR; Western blot analysis
• Experiment for Drug Resistance: MTT assay
• Mechanism Description: H19 overexpression induces resistance to 1,25(OH)2D3 by inhibiting the expression of VDR Through miR675-5p in colon cancer cells. vdr signaling was able to attenuate the proliferation and migration of colon cancer cells via multiple mechanisms including inhibiting Wnt/beta-catenin pathway, VDR signaling inhibits the expression of h19 by regulating the C-Myc/mad-1 Network.

References

• Ref 1: H19 Overexpression Induces Resistance to 1,25(OH)2D3 by Targeting VDR Through miR-675-5p in Colon Cancer Cells. Neoplasia. 2017 Mar;19(3):226-236. doi: 10.1016/j.neo.2016.10.007. Epub 2017 Feb 8.