Retifanlimab

Interactions

Retifanlimab interacts in the following cases:

Corticosteroids, immunosuppressants

The use of systemic corticosteroids or immunosuppressants before starting retifanlimab, except for physiological doses of systemic corticosteroids (≤10 mg/day prednisone or equivalent), should be avoided because of their potential interference with the pharmacodynamic activity and efficacy of retifanlimab. However, systemic corticosteroids or other immunosuppressants can be used after starting retifanlimab to treat immune-related adverse reactions.

Severe renal impairment

There is insufficient data in patients with severe renal impairment (creatinine clearance <30 mL/min) and no data for patients with end-stage renal disease and therefore no dosing recommendation can be mad.

Moderate or severe hepatic impairment

There are insufficient data in patients with moderate hepatic impairment and no data in patients with severe hepatic impairment and therefore no dosing recommendations can be made.

Allogeneic haematopoietic stem cell transplant

Fatal and other serious complications can occur in patients who receive allogeneic haematopoietic stem cell transplantation (HSCT) before or after being treated with a PD-1/PD-L1–blocking antibody. Transplant-related complications include hyperacute graft-versus-host disease (GvHD), acute GvHD, chronic GvHD, hepatic veno-occlusive disease after reduced intensity conditioning and steroid-requiring febrile syndrome (without an identified infectious cause). These complications may occur despite intervening therapy between PD-1/PD-L1 blockade and allogeneic HSCT. Patients should be closely followed for evidence of transplant-related complications and prompt intervention may be required. Consider the benefit versus risks of treatment with a PD-1/PD-L1–blocking antibody prior to or after an allogeneic HSCT.

Solid organ transplantation

Solid organ transplant rejection has been reported in the post-marketing setting in patients treated with PD-1 inhibitors. Treatment with retifanlimab may increase the risk of rejection in solid organ transplant recipients. The benefit of treatment with retifanlimab versus the risk of possible organ rejection should be considered in these patients.

Pregnancy

There are no data from the use of retifanlimab in pregnant women. Animal reproduction studies have not been conducted with retifanlimab. Animal studies have demonstrated that inhibition of the PD-1/PD-L1 pathway can lead to increased risk of immune-mediated rejection of the developing foetus resulting in foetal death. Therefore, based on its mechanism of action, retifanlimab can cause foetal harm when administered to a pregnant woman. Human IgG4 immunoglobulins are known to cross the placenta; therefore, retifanlimab has the potential to be transmitted from the mother to the developing foetus. Retifanlimab is not recommended during pregnancy and in women of childbearing potential not using effective contraception.

Nursing mothers

It is unknown whether retifanlimab is excreted in human milk. There is insufficient information on the excretion of retifanlimab in animal milk.

Human IgGs are known to be excreted in breast milk during the first few days after birth; which decreases to low concentrations soon afterwards; consequently, a risk to the breast-fed infant cannot be excluded during this short period. For this specific period, a decision should be made whether to discontinue/abstain from retifanlimab therapy, taking into account the benefit of breast-feeding to the child and the benefit of therapy to the woman. Afterwards, retifanlimab could be used during breast-feeding if clinically needed.

Carcinogenesis, mutagenesis and fertility

Women of childbearing potential/Contraception

Women of childbearing potential should use effective contraception during treatment with retifanlimab and for at least 4 months after the last dose of retifanlimab.

Fertility

No clinical data are available on the possible effects of retifanlimab on fertility. Animal reproduction studies to evaluate the effect of retifanlimab on fertility have not been conducted.

Effects on ability to drive and use machines

Retifanlimab has minor influence on the ability to drive and use machines. Because of potential adverse reactions such as fatigue, patients should be advised to use caution when driving or operating machinery until they are certain that retifanlimab does not adversely affect them.

Adverse reactions


Summary of the safety profile

Immune-related adverse reactions occurred with retifanlimab. Most of these, including severe reactions, resolved following initiation of appropriate medical therapy or withdrawal of retifanlimab (see "Description of selected adverse reactions" below).

The safety of retifanlimab as monotherapy has been evaluated in 452 patients with advanced solid malignancies who received the recommended 500 mg every 4 weeks dose, including 107 patients with metastatic or recurrent locally advanced MCC. Median duration of treatment was 5.4 months (range, 1 day – 27 months). The most common adverse reactions were fatigue (35.4%), rash (18.8%), diarrhoea (18.6%), anaemia (16.2%), pruritus (15.9%), arthralgia (13.3%), constipation (13.3%), nausea (13.3%), pyrexia (13.1%) and decreased appetite (12.6%). Adverse reactions were serious in 11.7% of patients; most serious adverse reactions were immune-related adverse reactions. Retifanlimab was permanently discontinued due to adverse reactions in 8% of patients; most of them were immune-related events.

The safety of retifanlimab in combination with carboplatin and paclitaxel has been evaluated in 154 patients with metastatic or with inoperable locally recurrent SCAC. Median duration of retifanlimab treatment was 7.4 months (range, 1 day – 14.6 months). The most common adverse reactions were neutropenia (70.1%), pruritus (24%), rash (23.4%), lymphopenia (14.3%), hypothyroidism (14.3%), and alanine aminotransferase increased (10.4%). Adverse reactions were serious in 13.6% of patients; most serious adverse reactions were immune-related adverse reactions. Retifanlimab was permanently discontinued due to adverse reactions in 5.8% of patients; most of them were immune-related events.

Tabulated list of adverse reactions

Adverse reactions reported in the pooled dataset for patients treated with retifanlimab monotherapy (N=452) and in combination with carboplatin and paclitaxel (N=154) are presented in the table below.

These reactions are presented by system organ class and by frequency. Frequencies are defined as: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1 000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000); and not known (cannot be estimated from the available data). Within each frequency grouping, adverse reactions are presented in order of decreasing incidence.

Adverse reactions in patients treated with retifanlimab:

 Retifanlimab monotherapy
(N=452)
Retifanlimab in combination with
carboplatin and paclitaxel
(N=154)
System organ classFrequency of all
grades
Frequency of grades
3-4
Frequency of all
grades
Frequency of grades
3-4
Blood and lymphatic
system disorders
Very common
Anaemiaa
Common
Anaemiaa
Very common
Lymphopeniab
Neutropeniac
Very common
Neutropeniac

Common
Lymphopeniab
Endocrine disordersCommon
Hypothyroidism,
Hyperthyroidism

Uncommon
Adrenal insufficiency
Thyroiditisd
Hypophysitis
Type 1 diabetes
mellituse
Uncommon
Adrenal insufficiency
Hypophysitis
Type 1 diabetes
mellituse
Very common
Hypothyroidism

Common
Adrenal insufficiency
Hyperthyroidism
Hypophysitis
Hyperglycaemia

Uncommon
Autoimmune
thyroiditis
Secondary
adrenocortical
insufficiency
Common
Adrenal insufficiency

Uncommon
Hypothyroidism
Hyperthyroidism
Secondary
adrenocortical
insufficiency
Metabolism and
nutrition disorders
Very common
Decreased appetite
Uncommon
Decreased appetite
Common
Hyponatraemia
Common
Hyponatraemia
Nervous system
disorders
Common
Paraesthesia

Uncommon
Polyneuropathyf
Radiculopathy
Vocal cord paralysis
Uncommon
Polyneuropathyf
Radiculopathy
Very common
Peripheral sensory
neuropathy

Common
Peripheral motor
neuropathy
Peripheral
sensorimotor
neuropathy
Common
Peripheral
sensorimotor
neuropathy
Eye disordersUncommon
Uveitisg
Keratitis
Uncommon
Uveitisg
  
Cardiac disordersUncommon
Pericarditis
Myocarditis
Uncommon
Myocarditis
  
Respiratory, thoracic
and mediastinal
disorders
Common
Pneumonitish
Uncommon
Pneumonitish
  
Gastrointestinal
disorders
Very common
Diarrhoea
Nausea
Constipation

Common
Colitisi

Uncommon
Pancreatitis
Uncommon
Diarrhoea
Pancreatitis
Colitisi
Very common
Colitisj

Common
Stomatitis
Common
Colitisj
Hepatobiliary
disorders
Common
Hepatocellular injury
Hepatitisk

Uncommon
Hyperbilirubinaemia
Cholangitis
Uncommon
Hepatitisk
Hepatocellular injury
Cholangitis
Hyperbilirubinaemia
Common
Hepatitisl

Uncommon
Immune-mediated
cholangitis
Common
Hepatitisl

Uncommon
Immune-mediated
cholangitis
Skin and
subcutaneous skin
disorders
Very common
Rashm
Pruritus
Common
Rashm
Very common
Pruritus
Rashn
Common
Rashn

Uncommon
Pruritus
Musculoskeletal and
connective tissue
disorders
Very common
Arthralgia

Uncommon
Arthritis°
Myositis
Eosinophilic fasciitis
Polymyalgia
rheumatica
Uncommon
Arthralgia
Arthritis°
Myositis
Eosinophilic fasciitis
Common
Arthritis
 
Renal and urinary
disorders
Common
Acute kidney injury
Renal failure

Uncommon
Tubulointerstitial
nephritis
Uncommon
Acute kidney injury
Tubulointerstitial
nephritis
  
General disorders
and administration
site conditions
Very common
Fatiguep
Pyrexia
Common
Fatiguep

Uncommon
Pyrexia
Very common
Asthenia
Common
Asthenia
InvestigationsCommon
Transaminases
increasedq
Blood creatinine
increased
Amylase increased
Lipase increased
Blood bilirubin
increased
Blood thyroid
stimulating hormone
increased

Uncommon
Blood thyroid
stimulating hormone
decreased
Common
Transaminases
increasedq

Uncommon
Blood bilirubin
increased
Lipase increased
Blood creatinine
increased
Amylase increased
Very common
Alanine
aminotransferase
increased

Common
Aspartate
aminotransferase
increased
Lipase increased
Blood creatinine
increased
Amylase increased
Common
Alanine
aminotransferase
increased
Aspartate
aminotransferase
increased
Lipase increased

Uncommon
Blood creatinine
increased
Amylase increased
Injury, poisoning
and procedural
complications
Common
Infusion-related
reactionr
Uncommon
Infusion-related
reactionr
Common
Infusion-related
reaction
Uncommon
Infusion-related
reaction

a Includes anaemia, iron deficiency anaemia, anaemia of malignant disease and anaemia vitamin B12 deficiency.
b Includes lymphopenia and lymphocyte count decreased.
c Includes neutropenia and neutrophil count decreased.
d Includes thyroiditis and autoimmune thyroiditis.
e Includes diabetic ketoacidosis.
f Includes polyneuropathy and demyelinating polyneuropathy.
g Includes uveitis and iritis.
h Includes pneumonitis, interstitial lung disease, organising pneumonia and lung infiltration.
i Includes colitis and immune mediated enterocolitis.
j Includes colitis, immune mediated enterocolitis and immune mediated diarrhoea.
k Includes hepatitis and autoimmune hepatitis.
l Includes hepatitis and immune-mediated hepatitis.
m Includes rash, rash maculo-papular, rash erythematous, rash pruritic, dermatitis, psoriasis, rash macular, rash papular, lichenoid keratosis, rash pustular, dermatitis bullous, palmar-plantar erythrodyseasthesia syndrome, toxic epidermal necrolysis and toxic skin eruption.
n Includes rash, rash erythematous, rash maculo-papular and rash pruritic.
° Includes arthritis and polyarthritis.
p Includes asthenia and fatigue.
q Includes transaminases increased, alanine aminotransferase increased and aspartate aminotransferase increased.
r Includes drug hypersensitivity and infusion related reaction.

Description of selected adverse reactions

The selected adverse reactions described below are based on the safety of retifanlimab monotherapy in a pooled safety population of 452 patients with advanced solid malignancies, including patients with metastatic or recurrent locally advanced MCC and on the safety of retifanlimab in combination with carboplatin and paclitaxel in 154 patients with metastatic or with inoperable locally recurrent SCAC. The management guidelines for these adverse reactions are described in section 4.2.

Immune-related adverse reactions

Immune-related pneumonitis

Immune-related pneumonitis occurred in 3.1% of patients receiving retifanlimab monotherapy, including 1.3% of patients with Grade 2, 0.9% of patients with Grade 3 and 0.2% of patients with Grade 5. The median time to onset of pneumonitis was 100 days (range, 43 – 673 days). Pneumonitis led to discontinuation of retifanlimab in 0.2% of patients. Among the patients with pneumonitis, 71.4% received systemic corticosteroids. Pneumonitis resolved in 78.6% of patients, with a median time to resolution of 37 days (range, 9 – 104 days).

Immune-related colitis

Immune-related colitis occurred in 2.7% of patients receiving retifanlimab monotherapy, including 1.1% of patients with Grade 2, 0.4% of patients with Grade 3 and 0.2% of patients with Grade 4. The median time to onset of colitis was 165.5 days (range, 11 – 749 days). Colitis led to discontinuation of retifanlimab in 0.9% of patients. Among the patients with colitis, 75% received systemic corticosteroids and 8.3% received another immunosuppressant (infliximab). Colitis resolved in 66.7% of patients, with a median time to resolution of 83.5 days (range, 15 – 675 days).

In patients with SCAC receiving retifanlimab in combination with carboplatin and paclitaxel, immune-related colitis occurred in 10.4% of patients, including 3.2% of patients with Grade 2, 2.6% of patients with Grade 3 and 0.6% of patients with Grade 4. The median time to onset of colitis was 83.5 days (range, 3 – 271 days). Colitis led to discontinuation of retifanlimab in 1.3% of patients. Among the patients with colitis, 93.8% received systemic corticosteroids and 6.3% received another immunosuppressant (infliximab). Colitis resolved in 93.8% of patients, with a median time to resolution of 27 days (range, 1 – 102 days).

Immune-related nephritis

Immune-related nephritis occurred in 2% of patients receiving retifanlimab monotherapy, including 0.4% of patients with Grade 2, 1.1% of patients with Grade 3 and 0.4% of patients with Grade 4. The median time to onset of nephritis was 176 days (range, 15 – 515 days). Nephritis led to discontinuation of retifanlimab in 1.1% of patients. Among the patients with nephritis, 66.7% received systemic corticosteroids. Nephritis resolved in 44.4% of patients, with a median time to resolution of 22.5 days (range, 9 – 136 days).

Immune-related endocrinopathies

Hypothyroidism occurred in 10.2% of patients receiving retifanlimab monotherapy, including 4.9% of patients with Grade 2. The median time to onset of hypothyroidism was 88 days (range, 1 – 505 days). None of the events led to discontinuation of retifanlimab. Hypothyroidism resolved in 32.6% of patients, with a median time to resolution of 56 days (range, 2 – 224 days).

In patients with SCAC receiving retifanlimab in combination with carboplatin and paclitaxel, hypothyroidism occurred in 14.3% of patients, including 9.1% of patients with Grade 2 and 0.6% of patients with Grade 4. The median time to onset of hypothyroidism was 138.5 days (range, 55 – 390 days). Hypothyroidism led to discontinuation of retifanlimab in 1 patient. Hypothyroidism resolved in 27.3% of patients, with a median time to resolution of 114 days (range, 57 – 212 days).

Hyperthyroidism occurred in 5.8% of patients receiving retifanlimab monotherapy, including 2.7% of patients with Grade 2. The median time to onset of hyperthyroidism was 55.5 days (range, 8 – 575 days). None of the events led to discontinuation of retifanlimab. Hyperthyroidism resolved in 61.5% of patients, with a median time to resolution of 74 days (range, 15 – 295 days).

In patients with SCAC receiving retifanlimab in combination with carboplatin and paclitaxel, hyperthyroidism occurred in 8.4% of patients, including 3.2% of patients with Grade 2 and 0.6% of patients with Grade 3. The median time to onset of hyperthyroidism was 82 days (range, 8 – 278 days). None of the events led to discontinuation of retifanlimab. Hyperthyroidism resolved in 76.9% of patients, with a median time to resolution of 29 days (range, 8 – 130 days).

Hypophysitis occurred in 0.7% of patients receiving retifanlimab monotherapy, including 0.4% of patients with Grade 2 and 0.2% of patients with Grade 3. The median time to onset of hypophysitis was 308 days (range, 266 – 377 days). Hypophysitis led to discontinuation of retifanlimab in 0.2% of patients. Hypophysitis resolved in 33.3% of patients, with a time to resolution of 6 days.

In patients with SCAC receiving retifanlimab in combination with carboplatin and paclitaxel, hypophysitis occurred in 2 patients (1.3%, both Grade 2). The median time to onset of hypophysitis was 192 days (range, 90 – 294 days). Neither of the events led to discontinuation of retifanlimab. Hypophysitis resolved in 1 of the 2 patients, with a time to resolution of 8 days.

Adrenal insufficiency occurred in 0.9% of patients receiving retifanlimab monotherapy, including 0.4% of patients with Grade 2 and 0.4% of patients with Grade 3. The median time to onset of adrenal insufficiency was 220.5 days (range, 146 – 275 days). None of the events led to discontinuation of retifanlimab. Adrenal insufficiency resolved in 25% of patients, with a time to resolution of 12 days.

In patients with SCAC receiving retifanlimab in combination with carboplatin and paclitaxel, adrenal insufficiency occurred in 5.8% of patients, including 1.9% of patients with Grade 2 and 1.9% of patients with Grade 3. The median time to onset of adrenal insufficiency was 197 days (range, 63 – 302 days). One event led to discontinuation of retifanlimab. Adrenal insufficiency resolved in 44.4% of patients, with a time to resolution of 13.5 days.

Type 1 diabetes mellitus presenting as diabetic ketoacidosis (Grade 3) occurred in 0.2% of patients receiving retifanlimab monotherapy. The time to onset of diabetic ketoacidosis was 284 days. The event did not lead to discontinuation of retifanlimab and resolved with a time to resolution of 6 days.

Immune-related hepatitis

Immune-related hepatitis occurred in 3.5% of patients receiving retifanlimab monotherapy, including 0.9% of patients with Grade 2, 2.4% of patients with Grade 3 and 0.2% of patients with Grade 4. The median time to onset of hepatitis was 70.5 days (range, 8 – 580 days). Hepatitis led to discontinuation of retifanlimab in 1.5% of patients. Among the patients with hepatitis, 81.3% of patients received systemic corticosteroids and 6.3% of patients received another immunosuppressant (mycophenolate mofetil). Hepatitis resolved in 56.3% of patients, with a median time to resolution of 22 days (range, 6 – 104 days).

In patients with SCAC receiving retifanlimab in combination with carboplatin and paclitaxel, immune-related hepatitis occurred in 2 patients (1.3%, both Grade 3). The median time to onset of hepatitis was 195.5 days (range, 140 – 251 days). Hepatitis led to discontinuation of retifanlimab in 1 patient. Both patients with hepatitis received systemic corticosteroids and another immunosuppressant (mycophenolate mofetil). Hepatitis resolved in both patients, with a median time to resolution of 58.5 days (range, 57 – 60 days).

Immune-related skin reactions

Immune-related skin reactions occurred in 9.5% of patients receiving retifanlimab monotherapy, including 8% of patients with Grade 2, 1.1% of patients with Grade 3 and 0.2% of patients with Grade 4. The median time to onset of skin reactions was 86 days (range, 2 – 589 days). Skin reactions led to discontinuation of retifanlimab in 0.7% of patients. Among the patients with skin reactions, 32.6% of patients received systemic corticosteroids. Skin reactions resolved in 72.1% of patients, with a median time to resolution of 37 days (range, 3 – 470 days).

In patients with SCAC receiving retifanlimab in combination with carboplatin and paclitaxel, immune-related skin reactions occurred in 11.7% of patients, including 9.7% of patients with Grade 2 and 1.9% of patients with Grade 3. The median time to onset of skin reactions was 46.5 days (range, 2 – 443 days). Skin reactions led to discontinuation of retifanlimab in 2 patients. Among the patients with skin reactions, 33.3% of patients received systemic corticosteroids. Skin reactions resolved in 72.2% of patients, with a median time to resolution of 22 days (range, 5 – 385 days).

Infusion related-reactions

Infusion-related reactions occurred in 6.2% of patients receiving retifanlimab monotherapy, including 2.2% of patients with Grade 2 and 0.4% of patients with Grade 3. Infusion-related reactions led to discontinuation of retifanlimab in 0.4% patients. In patients with SCAC receiving retifanlimab in combination with carboplatin and paclitaxel, infusion-related reactions occurred in 9.7% of patients, including 1.9% of patients with Grade 3. None of the infusion-related reactions led to discontinuation of retifanlimab.

Laboratory abnormalities

In patients with SCAC receiving retifanlimab in combination with chemotherapy, the proportion of patients who experienced a shift from baseline to a Grade 3 or 4 laboratory abnormality occurring in >3% of patients was 42.8% for decreased lymphocytes, 52% for decreased neutrophils, 4.5% for lipase, 3.9% for alanine aminotransferase, and 3.9% for aspartate aminotransferase.

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