GI50s are summarised in Table 1. Our cell panel consisted of LHRH receptor-positive (OVCAR-3) and receptor-negative (SK-OV-3) ovarian cancer cell lines used in Zoptarelin doxorubicin's preclinical development studies. Non-cancerous human ovarian (H-6036) and lung fibroblast (MRC-5) cell lines were also included for selectivity comparison. Paclitaxel, a first-line chemotherapeutic drug used for ovarian cancer, was observed to be highly cytotoxic against all cell lines, including non-cancerous ovarian and human fibroblasts (GI50s 1-5 nM). Unsurprisingly, common and serious side-effects experienced by more than 50% patients dosed with this drug included anaemia, neutropenia, peripheral neuropathy, nausea, vomiting, myalgia, arthralgia and alopecia. Similarly, doxorubicin was also shown to be non-specific towards all the cell lines (GI50s 60-311 nM), below the reported average 631 nM GI50 in a study involving 39 cancer cell lines. It is noteworthy that doxorubicin exhibited moderate GI50s of 311 and 218 nM against OVCAR-3 and SK-OV-3, respectively, supporting earlier in vitro data. Tubulin binder MMAE was found to be ultra-toxic against all cell lines (GI50s 0.5-1.1 nM), supporting the findings from an earlier report. It is therefore unsurprising that MMAE has never been approved as a drug on its own. The LHRH analog and carrier peptide, D-Cys6-LHRH, was inactive against all cell lines (GI50s >50,000 nM).

GI50s are summarised in Table 1. Our cell panel consisted of LHRH receptor-positive (OVCAR-3) and receptor-negative (SK-OV-3) ovarian cancer cell lines used in Zoptarelin doxorubicin's preclinical development studies. Non-cancerous human ovarian (H-6036) and lung fibroblast (MRC-5) cell lines were also included for selectivity comparison. Paclitaxel, a first-line chemotherapeutic drug used for ovarian cancer, was observed to be highly cytotoxic against all cell lines, including non-cancerous ovarian and human fibroblasts (GI50s 1-5 nM). Unsurprisingly, common and serious side-effects experienced by more than 50% patients dosed with this drug included anaemia, neutropenia, peripheral neuropathy, nausea, vomiting, myalgia, arthralgia and alopecia. Similarly, doxorubicin was also shown to be non-specific towards all the cell lines (GI50s 60-311 nM), below the reported average 631 nM GI50 in a study involving 39 cancer cell lines. It is noteworthy that doxorubicin exhibited moderate GI50s of 311 and 218 nM against OVCAR-3 and SK-OV-3, respectively, supporting earlier in vitro data. Tubulin binder MMAE was found to be ultra-toxic against all cell lines (GI50s 0.5-1.1 nM), supporting the findings from an earlier report. It is therefore unsurprising that MMAE has never been approved as a drug on its own. The LHRH analog and carrier peptide, D-Cys6-LHRH, was inactive against all cell lines (GI50s >50,000 nM).

GI50s are summarised in Table 1. Our cell panel consisted of LHRH receptor-positive (OVCAR-3) and receptor-negative (SK-OV-3) ovarian cancer cell lines used in Zoptarelin doxorubicin's preclinical development studies. Non-cancerous human ovarian (H-6036) and lung fibroblast (MRC-5) cell lines were also included for selectivity comparison. Paclitaxel, a first-line chemotherapeutic drug used for ovarian cancer, was observed to be highly cytotoxic against all cell lines, including non-cancerous ovarian and human fibroblasts (GI50s 1-5 nM). Unsurprisingly, common and serious side-effects experienced by more than 50% patients dosed with this drug included anaemia, neutropenia, peripheral neuropathy, nausea, vomiting, myalgia, arthralgia and alopecia. Similarly, doxorubicin was also shown to be non-specific towards all the cell lines (GI50s 60-311 nM), below the reported average 631 nM GI50 in a study involving 39 cancer cell lines. It is noteworthy that doxorubicin exhibited moderate GI50s of 311 and 218 nM against OVCAR-3 and SK-OV-3, respectively, supporting earlier in vitro data. Tubulin binder MMAE was found to be ultra-toxic against all cell lines (GI50s 0.5-1.1 nM), supporting the findings from an earlier report. It is therefore unsurprising that MMAE has never been approved as a drug on its own. The LHRH analog and carrier peptide, D-Cys6-LHRH, was inactive against all cell lines (GI50s >50,000 nM).

GI50s are summarised in Table 1. Our cell panel consisted of LHRH receptor-positive (OVCAR-3) and receptor-negative (SK-OV-3) ovarian cancer cell lines used in Zoptarelin doxorubicin's preclinical development studies. Non-cancerous human ovarian (H-6036) and lung fibroblast (MRC-5) cell lines were also included for selectivity comparison. Paclitaxel, a first-line chemotherapeutic drug used for ovarian cancer, was observed to be highly cytotoxic against all cell lines, including non-cancerous ovarian and human fibroblasts (GI50s 1-5 nM). Unsurprisingly, common and serious side-effects experienced by more than 50% patients dosed with this drug included anaemia, neutropenia, peripheral neuropathy, nausea, vomiting, myalgia, arthralgia and alopecia. Similarly, doxorubicin was also shown to be non-specific towards all the cell lines (GI50s 60-311 nM), below the reported average 631 nM GI50 in a study involving 39 cancer cell lines. It is noteworthy that doxorubicin exhibited moderate GI50s of 311 and 218 nM against OVCAR-3 and SK-OV-3, respectively, supporting earlier in vitro data. Tubulin binder MMAE was found to be ultra-toxic against all cell lines (GI50s 0.5-1.1 nM), supporting the findings from an earlier report. It is therefore unsurprising that MMAE has never been approved as a drug on its own. The LHRH analog and carrier peptide, D-Cys6-LHRH, was inactive against all cell lines (GI50s >50,000 nM).