Introduction
Target | Drug | Half-life | Regimen | Indication | First approved doses | Current approved doses |
---|---|---|---|---|---|---|
CTLA-4 | Ipilimumab | ~15 days | Monotherapy | Advanced melanoma | 3 mg/kg Q3W total of 4 doses | |
Monotherapy | Adjuvant melanoma* | 10 mg/kg Q3W for 4 doses followed by 10 mg/kg Q12W up to 3 years | ||||
In combination with nivolumab | Advanced melanoma HCC* | 3 mg/kg Q3W total of 4 doses | ||||
Advanced RCC MSI-H/dMMr mCRC | 1 mg/kg Q3W total of 4 doses | |||||
mNSCLC* mesothelioma | 1 mg/kg Q6W up to 2 years | |||||
In combination with nivolumab and chemotherapy | mNSCLC | 1 mg/kg Q6W up to 2 years | ||||
PD-1 | Nivolumab | ~25 days | Monotherapy | Advanced melanoma mNSCLC Advanced RCC Hodgkin lymphoma HNSCC Urothelial carcinoma HCC* Esophageal cancer MSI-H/dMMr mCRC* | 3 mg/kg Q2W | 240 mg Q2W or 480 mg Q4W† |
Adjuvant melanoma Adjuvant Esophageal or GEJ cancer | 240 mg Q2W or 480 mg Q4W† up to 1 year | |||||
MSI-H/dMMr mCRC (< 40 kg)* | 3 mg/kg Q2W | |||||
In combination with ipilimumab | Advanced melanoma HCC* | 1 mg/kg Q3W for 4 doses followed by 3 mg/kg Q2W | 1 mg/kg Q3W for 4 doses followed by 240 mg Q2W or 480 mg Q4W | |||
mNSCLC* | 3 mg/kg Q2W up to 2 years | |||||
Mesothelioma | 3 mg/kg Q2W | 360 mg Q3W up to 2 years | ||||
Advanced RCC MSI-H/dMMr mCRC | 3 mg/kg Q3W for 4 doses followed by 3 mg/kg Q2W | 3 mg/kg Q3W for 4 doses followed by 240 mg Q2W or 480 mg Q4W | ||||
MSI-H/dMMr mCRC (< 40 kg) | 3 mg/kg Q2W | |||||
In combination with ipilimumab and chemotherapy | mNSCLC | 360 mg Q3W up to 2 years | ||||
In combination with cabozantinib | Advanced RCC | 240 mg Q2W up to 2 years | 240 mg Q2W or 480 mg Q4W up to 2 years | |||
In combination with chemotherapy | Gastric, GEJ, Esophageal cancer* | 240 mg Q2W or 360 mg Q3W up to 2 years | ||||
Pembrolizumab | ~25 days | Monotherapy | Advanced melanoma mNSCLC mSCLC* Hodgkin lymphoma Mediastinal B-cell lymphoma* HNSCC Urothelial carcinoma HCC* Gastric, GEJ, Esophageal cancer* Cervical cancer* Merkel cell carcinoma* MSI-H/dMMr mCRC High-risk NMIBC* Cutaneous SCC* | 2 mg/kg Q3W up to 2 years | 200 mg Q3W or 400 mg Q6W up to 2 years | |
Adjuvant melanoma | 200 mg Q3W up to 1 year | 200 mg Q3W or 400 mg Q6W up to 1 year | ||||
Pediatrics | 2 mg/kg Q3W up to 2 years | |||||
In combination with chemotherapy | mNSCLC HNSCC Esophageal cancer Advanced TNBC* | 2 mg/kg Q3W up to 2 years | 200 mg Q3W or 400 mg Q6W up to 2 years | |||
In combination with trastuzumab and chemotherapy | Gastric, GEJ cancer* | |||||
In combination with axitinib | Advanced RCC | |||||
In combination with lenvatinib | Endometrial carcinoma* | |||||
Cemiplimab | ~19 days | Monotherapy | Cutaneous SCC BCC mNSCLC | 3 mg/kg Q2W | 350 mg Q3W | |
PD-L1 | Avelumab | ~4 days | Monotherapy | Metastatic Merkel cell carcinoma Urothelial cancer | 10 mg/kg Q2W | 800 mg Q2W |
In combination with axitinib | Advanced RCC | |||||
Atezolizumab | ~27 days | Monotherapy | Urothelial cancer mNSCLC | 1200 mg Q3W | 840 mg Q2W or 1200 mg Q3W or 1680 mg Q4W | |
In combination with nab-paclitaxel | Advanced TNBC | 840 mg Q2W | ||||
In combination with bevacizumab and chemotherapy | mNSCLC | 1200 mg Q3W | 840 mg Q2W* or 1200 mg Q3W or 1680 mg Q4W* | |||
In combination with chemotherapy | mSCLC | |||||
In combination with bevacizumab | HCC | |||||
In combination with cobimetinib and vemurafenib | Advanced melanoma* | |||||
Durvalumab | ~18 days | Monotherapy | Unresectable NSCLC | 10 mg/kg Q2W up to 1 year | 10 mg/kg Q2W or 1500 mg Q4W up to 1 year | |
Patients < 30 kg | 10 mg/kg Q2W up to 1 year | |||||
In combination with chemotherapy | Extensive-stage SCLC | 1500 mg Q3W for 4 doses followed by 1500 mg Q4W | 1500 mg Q3W for 4 doses followed by 1500 mg Q4W | |||
Patients < 30 kg | 20 mg/kg Q3W for 4 doses followed by 10 mg/kg Q2W |
Target | Drug | Indication | Dose | ORR (%) | PFS (% at 24 weeks; otherwise median) | OS (% at 1 year; otherwise median or specified) | G3-G4 toxicity (%) |
---|---|---|---|---|---|---|---|
CTLA-4 | Melanoma | 3 mg/kg Q3W | [4.2–19] | 12.9% [2.63–2.9] months | [39.3–60.9]% | [15–27.3] | |
10 mg/kg Q3W | [11.1–15] | 18.9% [2.56–2.8] months | [44.2–54.3]% | [31–34] | |||
0.3 mg/kg Q3W | 0 | 2.7% | 39.6% | ||||
RCC | 1 mg/kg Q3W | 40.4 | 55.6% | 81% | 38.3 | ||
3 mg/kg Q3W | 40.4 | 63.8% | 85% | 61.7 | |||
PD-1 | Melanoma | 0.1 mg/kg Q2W | [29–35] | [40–41]% | [0–5] | ||
0.3 mg/kg Q2W | [19–28] | [31–35]% | [0–3] | ||||
1 mg/kg Q2W | [30 31] | [45–51]% | [6–12] | ||||
3 mg/kg Q2W | [31–43.7] | [39–55]% 6.9 months | 72.9% | [4–16.3] | |||
10 mg/kg Q2W | [9–20] | [30–45]% | [8–21] | ||||
NSCLC | 1 mg/kg Q2W | [3–6] | [26–46]% | 33% | 15.2 | ||
3 mg/kg Q2W | [24–32] | [40–41]% | 56% | 13.5 | |||
10 mg/kg Q2W | [18–20] | [24–33]% | 38% | 13.6 | |||
RCC | 0.3 mg/kg Q2W | 20 | 30% | 18.2% | 5 | ||
1 mg/kg Q2W | [24–28] | [47–50]% | 12 | ||||
2 mg/kg Q2W | 22 | 30% | 25.5% | 17 | |||
10 mg/kg Q2W | 31 | 67% | 24.7% | 13 | |||
Mixed | 480 mg Q4W | 14.8 | |||||
Melanoma | 2 mg/kg Q3W | [21–32.9] | 45% | 58% | [8–15] | ||
10 mg/kg Q2W | [33.7–52] | [13.3–22.8] | |||||
10 mg/kg Q3W | [26–35.9] | 37% | 53% | [3.6–16] | |||
NSCLC | 2 mg/kg Q3W | [15–25] | 3.9 months | 10.4 months | 13 | ||
10 mg/kg Q2W | [19.3–21] | 9 | |||||
10 mg/kg Q3W | [19.2–25] | 4 months | 12.7 months | [3.6–16] | |||
Hodgkin lymphoma | 10 mg/kg Q2W | 65 | 69% | 100% at 24 weeks | 22 | ||
200 mg Q3W | 69 | 5.4 | |||||
HNSCC | 10 mg/kg Q2W | 18 | 23 | ||||
200 mg Q3W | 16 | 23% | 59% at 24 weeks | 15 | |||
Urothelial cancer | 10 mg/kg Q2W | 26 | 2 months | 13 months | 15 | ||
200 mg Q3W | 24 | 2.1 months | 10.3 months | 15 | |||
Cemiplimab [32] | Cutaneaous SCC | 350 mg Q3W | 41 | 10.4 months | 76.1% | 39.3 | |
3 mg/kg Q2W | 49 | 18.4 months | 81.3% | 50.8 | |||
PD-L1 | RCC | 10 mg/kg Q2W | [51.4–58] | 13.8 months | [58–71.2] | ||
Merkel cell carcinoma | 10 mg/kg Q2W | 31.8 | 40% | 69% at 24 weeks | 5 | ||
Mixed | 1 mg/kg Q2W | 0 | 25 | ||||
3 mg/kg Q2W | 0 | 0 | |||||
10 mg/kg Q2W | 13 | 33 | |||||
20 mg/kg Q2W | 10 | 14 | |||||
NSCLC | 1200 mg Q3W | 14 | 2.8 months | 13.8 months | 13 | ||
1; 3; 10; 15, 20 mg/kg Q3W | 23 | 45% | |||||
Melanoma | 30 | 41% | |||||
RCC | 14 | 48% | |||||
Urothelial cancer | 1200 mg Q3W | 15 | 2.1 months | 7.9 months | 16 | ||
SCLC | 1500 mg Q3W | 68 | 45% | 54% | 22 | ||
Urothelial cancer | 10 mg/kg Q2W | 31 | 5 | ||||
NSCLC | 3 mg/kg Q2W | 0 | 0 | ||||
10 mg/kg Q2W | 33 | 67 | |||||
15 mg/kg Q2W | 33 | 72 | |||||
20 mg/kg Q2W | 50 | 61 | |||||
10 mg/kg Q2W | 0 | 17.2 months | 83.1% | [30.5–53] |