Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00302
|
|||||
|---|---|---|---|---|---|---|
| PDC Name |
PEN-221
|
|||||
| PDC Status |
Phase 2
|
|||||
| Indication |
In total 1 Indication(s)
Small cell lung cancer
|
|||||
| Structure |
|
|||||
| Peptide Name |
[Tyr3,Cys8] Octreotate amide
|
Peptide Info | ||||
| Receptor Name |
Somatostatin receptor type 2 (SSTR2)
|
Receptor Info | ||||
| Drug Name |
Mertansine DM1
|
Drug Info | ||||
| Therapeutic Target |
Microtubule (MT)
|
Target Info | ||||
| Linker Name |
Disulfide bond
|
Linker Info | ||||
| Formula |
C83H109ClN14O20S4
|
|||||
| #Ro5 Violations (Lipinski): 4 | Molecular Weight | 1786.584 | ||||
| Lipid-water partition coefficient (xlogp) | 3.312 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 15 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 26 | |||||
| Rotatable Bond Count (rotbonds) | 27 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Small cell lung cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 µmol/L
|
|||
| Administration Time | 6 h | ||||
| Description |
PEN-221 receptor dependent activity in vitro varied from strong (NCI-H524) to modest (HCC-33) but was consistent (N = 3) and correlated with in vivo activity (described below). Octreotide alone did not have an effect on cellular growth. These cell lines also demonstrated sensitivity to the cytotoxic payload, DM1, with sub-micromolar IC50's after a 6-hour exposure and 70-hour additional incubation period (Supplementary Fig. S2B).
Click to Show/Hide
|
||||
| In Vitro Model | Lung small cell carcinoma | NCI-H524 cell | CVCL_1568 | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Small cell lung cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.108 µmol/L
|
|||
| Administration Time | 6 h | ||||
| Description |
PEN-221 receptor dependent activity in vitro varied from strong (NCI-H524) to modest (HCC-33) but was consistent (N = 3) and correlated with in vivo activity (described below). Octreotide alone did not have an effect on cellular growth. These cell lines also demonstrated sensitivity to the cytotoxic payload, DM1, with sub-micromolar IC50's after a 6-hour exposure and 70-hour additional incubation period (Supplementary Fig. S2B).
Click to Show/Hide
|
||||
| In Vitro Model | Small cell lung carcinoma | NCI-H69 cell | CVCL_1579 | ||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Small cell lung cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.258 µmol/L
|
|||
| Administration Time | 6 h | ||||
| Description |
PEN-221 receptor dependent activity in vitro varied from strong (NCI-H524) to modest (HCC-33) but was consistent (N = 3) and correlated with in vivo activity (described below). Octreotide alone did not have an effect on cellular growth. These cell lines also demonstrated sensitivity to the cytotoxic payload, DM1, with sub-micromolar IC50's after a 6-hour exposure and 70-hour additional incubation period (Supplementary Fig. S2B).
Click to Show/Hide
|
||||
| In Vitro Model | Small cell lung carcinoma | NCI-H69 cell | CVCL_1579 | ||
| Experiment 4 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Small cell lung cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.333 µmol/L
|
|||
| Administration Time | 6 h | ||||
| Description |
PEN-221 receptor dependent activity in vitro varied from strong (NCI-H524) to modest (HCC-33) but was consistent (N = 3) and correlated with in vivo activity (described below). Octreotide alone did not have an effect on cellular growth. These cell lines also demonstrated sensitivity to the cytotoxic payload, DM1, with sub-micromolar IC50's after a 6-hour exposure and 70-hour additional incubation period (Supplementary Fig. S2B).
Click to Show/Hide
|
||||
| In Vitro Model | Lung small cell carcinoma | NCI-H524 cell | CVCL_1568 | ||
| Experiment 5 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Small cell lung cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.658 µmol/L
|
|||
| Administration Time | 6 h | ||||
| Description |
PEN-221 receptor dependent activity in vitro varied from strong (NCI-H524) to modest (HCC-33) but was consistent (N = 3) and correlated with in vivo activity (described below). Octreotide alone did not have an effect on cellular growth. These cell lines also demonstrated sensitivity to the cytotoxic payload, DM1, with sub-micromolar IC50's after a 6-hour exposure and 70-hour additional incubation period (Supplementary Fig. S2B).
Click to Show/Hide
|
||||
| In Vitro Model | Lung small cell carcinoma | HCC33 cell | CVCL_2058 | ||
| Experiment 6 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Small cell lung cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.83 µmol/L
|
|||
| Administration Time | 6 h | ||||
| Description |
PEN-221 receptor dependent activity in vitro varied from strong (NCI-H524) to modest (HCC-33) but was consistent (N = 3) and correlated with in vivo activity (described below). Octreotide alone did not have an effect on cellular growth. These cell lines also demonstrated sensitivity to the cytotoxic payload, DM1, with sub-micromolar IC50's after a 6-hour exposure and 70-hour additional incubation period (Supplementary Fig. S2B).
Click to Show/Hide
|
||||
| In Vitro Model | Lung small cell carcinoma | HCC33 cell | CVCL_2058 | ||
References