Drug Information
General Information of This Drug
| Drug ID | DRG00041 | |||||
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| Drug Name | 12Adt-asp | |||||
| Synonyms |
12Adt-asp; Aspartyl-12adt; UNII-U4U7MXY86U; U4U7MXY86U; 1172636-20-2; CHEMBL4802225; C21580; Q27290687
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| Target(s) | Calcium-transporting ATPase type 2C member 1 (ATP2C1) | Target Info | ||||
| Structure |
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| Formula |
C46H72N2O15
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| #Ro5 Violations (Lipinski): 3 | Molecular Weight (mw) | 893.1 | ||||
| Lipid-water partition coefficient (xlogp) | 2.7 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 5 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 16 | |||||
| Rotatable Bond Count (rotbonds) | 30 | |||||
| PubChem CID | ||||||
| Canonical smiles |
CCCCCCCC(=O)OC1C2C(=C(C1OC(=O)C(=CC)C)C)C3C(C(CC2(C)OC(=O)C)OC(=O)CCCCCCCCCCCNC(=O)CC(C(=O)O)N)(C(C(=O)O3)(C)O)O
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| InChI |
InChI=1S/C46H72N2O15/c1-8-10-11-17-20-24-35(52)60-39-37-36(29(4)38(39)61-42(55)28(3)9-2)40-46(58,45(7,57)43(56)62-40)32(27-44(37,6)63-30(5)49)59-34(51)23-21-18-15-13-12-14-16-19-22-25-48-33(50)26-31(47)41(53)54/h9,31-32,37-40,57-58H,8,10-27,47H2,1-7H3,(H,48,50)(H,53,54)/b28-9-/t31-,32-,37+,38-,39-,40-,44-,45+,46+/m0/s1
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| InChIKey |
JFUXBZKLZFCZME-WFETZLHTSA-N
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| IUPAC Name |
(2S)-4-[[12-[[(3S,3aR,4S,6S,6aR,7S,8S,9bS)-6-acetyloxy-3,3a-dihydroxy-3,6,9-trimethyl-8-[(Z)-2-methylbut-2-enoyl]oxy-7-octanoyloxy-2-oxo-4,5,6a,7,8,9b-hexahydroazuleno[4,5-b]furan-4-yl]oxy]-12-oxododecyl]amino]-2-amino-4-oxobutanoic acid
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Each Peptide-drug Conjugate Related to This Drug
Full Information of The Activity Data of The PDC(s) Related to This Drug
Mipsagargin [Discontinued]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Time to disease progression | 134 Day | |||
| Patients Enrolled |
Patients with hepatocellular carcinoma who progressed on or after treatment with sorafenib or intolerant of sorafenib.
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| Administration Time | Days 1, 2, and 3 of a 28-day cycle | ||||
| Administration Dosage | 40 mg/m2 | ||||
| Description |
The median TTP was 134.0 days, median PFS was 129.0 days, and median OS was 205.0 days.
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| Experiment 2 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Non-small cell lung cancer | ||||
| Efficacy Data | Progression-free survival (PFS) | 52 day | |||
| Patients Enrolled |
Patients with non-small cell lung cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 10 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 3 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Pancreatic cancer | ||||
| Efficacy Data | Progression-free survival (PFS) | 57 day | |||
| Patients Enrolled |
Patients with pancreas cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 40 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 4 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Adenocarcinoma | ||||
| Efficacy Data | Progression-free survival (PFS) | 63 day | |||
| Patients Enrolled |
Patients with adenocarcinoma cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 66.8 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 5 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Advanced solid tumour | ||||
| Efficacy Data | Progression-free survival (PFS) | 77 day | |||
| Patients Enrolled |
Patients with endometrial cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 40/66.8/66.8 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 6 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Cholangiocarcinoma | ||||
| Efficacy Data | Progression-free survival (PFS) | 89 day | |||
| Patients Enrolled |
Patients with cholangiocarcinoma cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 2.5 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 7 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Prostate cancer | ||||
| Efficacy Data | Progression-free survival (PFS) | 112 day | |||
| Patients Enrolled |
Patients with prostate cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 1.2 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 8 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Colorectal cancer | ||||
| Efficacy Data | Progression-free survival (PFS) | 112 day | |||
| Patients Enrolled |
Patients with colorectal cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 5 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 9 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Prostate cancer | ||||
| Efficacy Data | Progression-free survival (PFS) | 119 day | |||
| Patients Enrolled |
Patients with prostate cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 88 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 10 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Prostate cancer | ||||
| Efficacy Data | Progression-free survival (PFS) | 121 day | |||
| Patients Enrolled |
Patients with prostate cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 40/66.8/66.8 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 11 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Progression-free survival (PFS) | 133 day | |||
| Patients Enrolled |
Patients with hepatocellular cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 40/66.8/66.8 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 12 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Progression-free survival (PFS) | 277 day | |||
| Patients Enrolled |
Patients with hepatocellular cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 40/66.8/66.8 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 13 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Progression-free survival (PFS) | 336 day | |||
| Patients Enrolled |
Patients with hepatocellular cancer.
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| Administration Time | Day 1/2/3 | ||||
| Administration Dosage | Dose level ( mg/m2) 40/66.8/66.8 | ||||
| Description |
Among the 42 patients considered to be evaluable for efficacy, there were no observations of objective response. However, 12 (28.6%) of patients had disease stabilisation. Overall, PFS was a median of 52.0 days (n1/442; censored 8; Q1, Q3: 50.0, 112.0). However, among the 12 patients with SD as best response, progression-free survival (PFS) was considerably higher: 129 days with 8 patients censored at the date of last study visit (Table 5A). Among the 16 efficacy-evaluable patients enrolled in part 2, 5 patients presented to the study with a diagnosis of hepatocellular carcinoma and had progressed on or were intolerant of sorafenib. In these 5 patients, prolonged disease stabilisation with an average PFS of 166 days (6 months) was observed (Table 5B); in patients with HCC who received more than 2 cycles of treatment, the PFS was 209 days, approaching 7.5 months
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| Experiment 14 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Progression-free survival (PFS) | 129 | |||
| Patients Enrolled |
Patients with hepatocellular carcinoma who progressed on or after treatment with sorafenib or intolerant of sorafenib.
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| Administration Time | Days 1, 2, and 3 of a 28-day cycle | ||||
| Administration Dosage | 40 mg/m2 | ||||
| Description |
The median TTP was 134.0 days, median PFS was 129.0 days, and median OS was 205.0 days.
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| Experiment 15 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Median overall survival (mOS) | 205 | |||
| Patients Enrolled |
Patients with hepatocellular carcinoma who progressed on or after treatment with sorafenib or intolerant of sorafenib.
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| Administration Time | Days 1, 2, and 3 of a 28-day cycle | ||||
| Administration Dosage | 40 mg/m2 | ||||
| Description |
The median TTP was 134.0 days, median PFS was 129.0 days, and median OS was 205.0 days.
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References