| MDL | MFCD28098202 |
|---|---|
| Molecular Weight | 718.79 |
| Molecular Formula | C82H84N8O16 |
| SMILES | C[C@]1(/C2=C/C(N3)=C4C)C(C(/C=C(C(C)=C/5C=C)\NC5=C/C6=N/C(C(CCC(OC)=O)=C6C)=C\C3=C4CCC(O)=O)=N2)=CC=C(C(OC)=O)[C@H]1C(OC)=O.C[C@]7(/C8=C/C(N9)=C%10C)C(C(/C=C(C(C)=C/%11C=C)\NC%11=C/C%12=N/C(C(CCC(O)=O)=C%12C)=C\C9=C%10CCC(OC)=O)=N8)=CC=C(C(OC)=O)[C@H]7C(OC)=O |
Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis [1] . Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation [3] .
IC50: YAP-TEAD interaction
Verteporfin is specifically selected by PDX-cell screening. The concentrations to cause 50% growth inhibition (GI 50 ) for PhLO, PhLH, and PhLK are 228 nM, 395 nM, and 538 nM, respectively, whereas GI 50 for ALL-1, TCC-Y/sr, and NPhA1 are 3.93 µM, 2.11 µM, and 5.61 µM, respectively. GSH significantly reduces the sensitivity of 2 out of 3 PDX cells to verteporfin. Verteporfin reduces the mitochondrial membrane potential in PDX cells [1] . Verteporfin reduces the PTX-resistance on HCT-8/T cells by inhibiting YAP expression and combination therapy with verteporfin and NSC 125973 shows synergism on inhibition of YAP and cytotoxicity to HCT-8/T [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Verteporfin (10 mg/kg, c.s.c.) and BMS-354825 significantly reduces the leukemia cell ratio, and combined therapy further reduced the number of leukemia cells in the spleen [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00135837 | Novartis|QLT Inc. |
Age-Related Macular Degeneration
|
June 2003 | Phase 4 |
| NCT03033225 | Mayo Clinic|National Cancer Institute (NCI) |
Advanced Pancreatic Carcinoma|Locally Advanced Pancreatic Carcinoma|Metastatic Pancreatic Carcinoma|Pancreatic Neoplasm|Stage II Pancreatic Cancer AJCC v8|Stage IIA Pancreatic Cancer AJCC v8|Stage IIB Pancreatic Cancer AJCC v8|Stage III Pancreatic Cancer AJCC v8|Stage IV Pancreatic Cancer AJCC v8|Unresectable Pancreatic Carcinoma
|
December 6, 2016 | Phase 2 |
| NCT00007969 | QLT Inc.|National Cancer Institute (NCI) |
Melanoma (Skin)
|
October 2000 | Phase 1|Phase 2 |
| NCT00546936 | Barnes Retina Institute|Genentech, Inc. |
Presumed Ocular Histoplasmosis (POHS)
|
October 2007 | Phase 2 |
| NCT02702700 | Centre Hospitalier Universitaire Vaudois |
Pleural Effusion, Malignant
|
January 2016 | Phase 1 |
| NCT02457026 | Duke University|Bausch & Lomb Incorporated |
Neovascular Age-related Macular Degeneration
|
January 2016 | Not Applicable |
| NCT00002647 | Medical College of Wisconsin|National Cancer Institute (NCI) |
Brain and Central Nervous System Tumors|Metastatic Cancer
|
May 1994 | Phase 1 |
| NCT00049959 | QLT Inc.|Novartis |
Basal Cell Carcinoma|Nevoid Basal Cell Carcinoma Syndrome|Gorlin Syndrome
|
Phase 3 | |
| NCT00433017 | Novartis |
Macular Degeneration|Choroidal Neovascularization
|
May 2007 | Phase 2|Phase 3 |
| NCT00574093 | Fondazione G.B. Bietti, IRCCS |
Neovascular Age Related Macular Degeneration
|
January 2008 | Phase 2 |
| NCT01846273 | Novartis Pharmaceuticals|Novartis |
Age-related Macular Degeneration|Polypoidal Choroidal Vasculopathy
|
August 7, 2013 | Phase 4 |
| NCT00570193 | Mid-Atlantic Retina Consultations, Inc. |
Choroidal Neovascularization|Macular Degeneration
|
December 2006 | Phase 1|Phase 2 |
| NCT01325181 | Jang Won Heo|Novartis Korea Ltd.|Seoul National University Hospital |
Chronic Central Serous Chorioretinopathy
|
July 2009 | Phase 1|Phase 2 |
| NCT01922102 | Novartis Pharmaceuticals|Novartis |
Visual Impairment Due to Choroidal Neovascularization (CNV) Secondary to Pathologic Myopia (PM)
|
September 11, 2013 | Phase 3 |
| NCT03067051 | SpectraCure AB |
Recurrent Prostate Cancer
|
March 21, 2017 | Phase 1|Phase 2 |
| NCT00347399 | Asociación para Evitar la Ceguera en México |
Age Related Macular Degeneration
|
March 2006 | Phase 2 |
| NCT00729846 | California Retina Consultants|Novartis |
Age Related Macular Degeneration|Choroidal Neovascularization|Macular Edema
|
May 2006 | Phase 2 |
| NCT04075136 | Wake Forest University Health Sciences|Modulight |
Exudative Age Related Macular Degeneration
|
November 2022 | Phase 4 |
| NCT00390208 | Bay Area Retina Associates|QLT Inc. |
Age Related Macular Degeneration
|
August 2006 | Phase 2 |
| NCT00426998 | Retinal Consultants Medical Group |
Choroidal Neovascularization|Macular Degeneration
|
April 2006 | Phase 2 |
| NCT01019668 | Shin Kong Wu Ho-Su Memorial Hospital |
Central Serous Chorioretinopathy
|
November 2008 | Not Applicable |
| NCT01746875 | Norwegian University of Science and Technology |
Macular Degeneration|Retinal Detachment
|
February 2014 | Not Applicable |
| NCT00436553 | Novartis |
Macular Degeneration|Choroidal Neovascularization
|
February 2007 | Phase 3 |
| NCT00331435 | Ophthalmic PDT Study Group |
Age Related Macular Degeneration
|
June 2006 | Phase 4 |
| NCT00211445 | Manhattan Eye, Ear & Throat Hospital |
Chronic Central Serous Chorioretinopathy
|
July 2002 | Phase 2 |
| NCT02872064 | University College, London |
Breast Neoplasms
|
January 2013 | Not Applicable |
| NCT00403442 | Vitreous -Retina- Macula Consultants of New York|QLT Inc. |
Macular Degeneration
|
September 2006 | Phase 1 |
| NCT01256580 | Massachusetts Eye and Ear Infirmary |
Choroidal Neovascularization|Myopia|Punctate Inner Choroidopathy (PIC)|Multifocal Choroiditis|Ocular Histoplasmosis Syndrome|Central Serous Chorioretinopathy (CSC)|Angioid Streaks|Trauma, or Hereditary Eye Diseases
|
August 2010 | Not Applicable |
| NCT00527475 | Texas Retina Associates|Novartis |
Macular Degeneration
|
May 2007 | Phase 2 |
| NCT00359164 | University of British Columbia |
Macular Degeneration
|
July 2006 | Phase 2 |
| NCT00211419 | Manhattan Eye, Ear & Throat Hospital|Alcon Research |
Maculopathy, Age-Related
|
Phase 1 | |
| NCT01217944 | Novartis Pharmaceuticals|Novartis |
Pathological Myopia
|
October 2010 | Phase 3 |
| NCT03459144 | Sun Yat-sen University |
Polypoidal Choroidal Vasculopathy
|
December 1, 2012 | Not Applicable |
| NCT00473642 | Oklahoma State University Center for Health Sciences|Novartis |
Age-Related Maculopathy|Choroidal Neovascularization
|
May 2007 | Phase 4 |
| NCT05589974 | Helse Stavanger HF |
Central Serous Chorioretinopathy
|
October 1, 2022 | |
| NCT00390026 | St. Erik Eye Hospital |
Age-Related Macular Degeneration
|
November 2006 | Phase 3 |
| NCT04590664 | Emory University|National Cancer Institute (NCI) |
Glioblastoma|Recurrent Glioblastoma
|
January 15, 2021 | Phase 1|Phase 2 |
| NCT00674323 | Novartis |
Polypoidal Choroidal Vasculopathy
|
April 2008 | Phase 4 |
| NCT01570608 | The Ludwig Boltzmann Institute of Retinology and Biomicroscopic Laser Surgery |
Age Related Macular Degeneration
|
March 2007 | Phase 3 |
| NCT00242580 | Novartis Pharmaceuticals|QLT Inc.|Novartis |
Macular Degeneration|Choroidal Neovascularization
|
September 2005 | Phase 3 |
| NCT02939274 | Rogers Sciences Inc. |
Metastatic Breast Cancer
|
October 2016 | Phase 2 |
| NCT00471406 | Chonnam National University Hospital |
Corneal Neovascularization
|
Not Applicable | |
| NCT00134667 | Eyetech Pharmaceuticals|Pfizer |
Age-Related Macular Degeneration
|
March 2005 | Phase 4 |
| NCT00492284 | QLT Inc. |
Choroidal Neovascularization|Macular Degeneration
|
July 2007 | Phase 2 |
Solid
Room temperature in continental US; may vary elsewhere.
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
DMSO : ≥ 200 mg/mL ( 278.25 mM )
DMF : 10 mg/mL ( 13.91 mM ; ultrasonic and warming and heat to 60°C)
* "≥" means soluble, but saturation unknown.
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.3912 mL | 6.9561 mL | 13.9123 mL |
| 5 mM | 0.2782 mL | 1.3912 mL | 2.7825 mL |
| 10 mM | 0.1391 mL | 0.6956 mL | 1.3912 mL |
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (6.96 mM); Clear solution